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Rimonabant (SR141716) Cannabinoid Receptor antagonist

Name: Rimonabant (SR141716)
Brand: Selleck Chemicals
SKU: S3021
Rating: 5 (8 reviews)

Cat.Nr.S3021

Rimonabant (SR141716) is een selectieve antagonist van CB1 met een IC50 van 13,6 nM en een EC50 van 17,3 nM in hCB1 getransfecteerde HEK 293-membraan, en het is ook een dubbele remmer van acyl CoA:cholesterol acyltransferases (ACAT) 1 en 2 die mycobacteriële MmpL3 remt.

Rimonabant (SR141716) Cannabinoid Receptor antagonist Chemical Structure

Chemische structuur

Moleculair gewicht: 463.79

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Kwaliteitscontrole

Batch: Zuiverheid: 99.67%

99.67

Gerelateerde doelwitten	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Overige Cannabinoid Receptor Inhibitoren	AM1241 AM251 BML-190 Otenabant (CP-945598) HCl 6-Iodopravadoline (AM630) Org 27569 GW842166X CID16020046 WIN 55, 212-2 mesylate Yangonin

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
CHO cells	Function assay			Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM	10465552
CHO	Function assay			Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM	14736243
CHO	Function assay			Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM	14736243
CHO	Function assay			Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM	14736243
CHO	Function assay			Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM	15713403
CHO	Function assay			In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM	15771428
CHO	Function assay			In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM	15771428
CHO	Function assay			In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM	15771428
CHO	Function assay			Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM	15801840
CHO	Function assay			Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM	16140010
CHO	Function assay			Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM	16140010
CHO	Function assay			Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM	16140010
CHOK1	Function assay			Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM	16263283
HEK293	Function assay			Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM	16263283
CHO	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM	16279809
HEK293	Function assay			Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM	17004712
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM	17004712
HEK293	Function assay			Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM	17004712
CHO	Function assay			Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM	17181138
CHO	Function assay			Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM	17181138
CHO	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM	17293109
CHO	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM	17293109
HEK293	Function assay			Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM	17383180
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM	17942307
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM	17942307
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM	17979261
CHOK1	Function assay			Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM	17979261
HEK293	Function assay			Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM	18083560
HEK293 EBNA	Function assay			Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM	18083560
HEK293	Function assay			Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM	18083560
CHOK1	Function assay			Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM	18243711
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM	18243711
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	18293908
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	18293908
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM	18335976
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM	18337096
CHO	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM	18342403
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM	18342403
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM	18363352
CHO	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM	18363352
SF9	Function assay			Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM	18448340
SF9	Function assay			Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM	18448340
SF9	Function assay			Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM	18448340
SF9	Function assay			Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM	18448340
HEK293	Function assay			Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM	18511157
CHO-K1	Function assay			Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM	18512901
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM	18512901
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM	18512901
CHO-K1	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM	18512901
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM	18579386
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	18579386
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM	18680276
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM	18680276
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM	18712856
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM	18712856
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM	18712856
HEK293	Function assay			Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control	18712856
CHO	Function assay			Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM	18800770
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM	18954042
CHO	Function assay			Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM	19022666
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM	19095444
HEK293	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM	19095444
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM	19095444
CHO-K1	Function assay			Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM	19102698
HEK293	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM	19102698
CHOK1	Function assay			Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM	19269817
CHOK1	Function assay			Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM	19328683
CHOK1	Function assay			Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM	19328683
HEK293	Function assay			Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM	19338356
HEK293	Function assay			Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM	19338356
CHOK1	Function assay		10 mins	Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM	19351113
HEK293	Function assay			Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM	19520572
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM	19530697
HEK293	Function assay			Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM	19530697
HEK293	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM	19530697
HEK293	Function assay	10 uM		Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level	19530697
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	19595596
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	19595596
CHO-K1	Function assay			Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM	19683918
CHO	Function assay			Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM	19850473
CHOK1	Function assay			Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM	19850473
CHO-K1	Function assay			Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM	19954978
CHO-K1	Function assay			Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM	20015647
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM	20015647
COS7	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM	20015647
CHO	Function assay			Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM	20045337
CHO	Function assay		60 mins	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM	20047779
CHO	Function assay		3 hrs	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM	20047779
CHO	Function assay		10 mins	Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM	20047779
CHO	Function assay		3 hrs	Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM	20047779
CHO	Function assay			Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM	20363132
CHO	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM	20363132
CHO	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM	20363132
CHO-K1	Function assay		1 hr	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM	20673729
HEK	Function assay			Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM	20718492
HEK	Function assay			Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM	20718492
CHO	Function assay			Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM	20845959
HEK293	Function assay			Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM	20845959
HEK293	Function assay			Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM	20845959
CHOK1	Function assay			Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM	20845959
HEK	Function assay			Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM	20943290
HEK	Function assay			Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM	20943290
CHO	Function assay			Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM	21334892
Sf9	Function assay			Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM	21334892
CHO	Function assay			Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM	21376588
HEK293	Function assay			Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM	21511945
HEK293	Function assay			Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM	21511945
HEK293	Function assay			Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG	21511945
HEK293	Function assay			Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG	21511945
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM	21702498
HEK	Function assay			Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM	21702498
CHO	Function assay		1 hr	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM	21741835
HEK293	Function assay		5 mins	Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM	21741835
CHO	Function assay		90 mins	Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM	21962575
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM	22372835
CHO-K1	Function assay			Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM	22372835
CHO-K1	Function assay			Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM	22372835
HEK	Function assay			Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM	22548457
HEK	Function assay			Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM	22548457
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM	22916707
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM	22916707
CHO	Function assay			Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM	22959249
CHO	Function assay		1 hr	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM	23072339
CHO	Function assay	> 0.1 nM	1 hr	Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry	23357307
N1E-115	Function assay	1 uM	5 mins	Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis	23357307
CHO	Function assay			Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM	23679955
HEK	Function assay		1 hr	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM	24175572
CHOK1	Function assay		1 hr	Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM	24175572
CHO	Function assay		45 mins	Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM	24445310
CHO	Function assay		45 mins	Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM	24445310
CHO-K1	Function assay		10 mins	Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM	24900484
HEK293	Function assay		60 mins	Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM	24900484
CHO-K1	Function assay		60 mins	Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM	24900484
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM	24900561
CHO	Function assay		2 hrs	Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM	24900561
CHO	Function assay		90 mins	Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM	24900561
RD-HGA16	Function assay			Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM	24944734
RD-HGA16	Function assay			Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM	24944734
Sf9	Function assay		20 mins	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM	25096297
Sf9	Function assay		20 mins	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM	25096297
CHO	Function assay			Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM	26151231
CHO	Function assay			Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM	26151231
HEK293	Function assay			Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay	26203658
HEK293	Function assay		90 mins	Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM	26756097
HEK293	Function assay		90 mins	Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM	26756097
CHO-K1	Function assay			Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM	26827137
CHO	Function assay		90 secs	Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM	26827137
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
CHOK1	Function assay		90 mins	Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM	29939744
HEK293	Function assay			Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM	30077609
HEK293	Function assay		90 secs	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM	30077609
HEK293	Function assay		30 mins	Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM	30339387
CHO	Function assay			Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM	31609608
CHO	Function assay			Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM	ChEMBL
CHO	Function assay			Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM	ChEMBL
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	463.79	Formule	C₂₂H₂₁Cl₃N₄O	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	168273-06-1	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	N/A			Smiles	CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl

Oplosbaarheid

In vitro
Batch:

DMSO : 92 mg/mL (198.36 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	5.000mg/ml (10.78mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Kenmerken	Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.
Targets/IC₅₀/Ki	ACAT1 ACAT2 MmpL3 hCB1 (Cell-free assay) 13.6 nM hCB2 (Cell-free assay) 1.64 μM
In vitro	Rimonabant (SR141716) vermindert dosisafhankelijk de ACAT-activiteit in Raw264.7-macrofagen met een IC50 van 2,9 μM en geïsoleerde peritoneale macrofagen. Het remt de ACAT-activiteit in intacte CHO-ACAT1- en CHO-ACAT2-cellen en in celvrije assays met een ongeveer gelijke efficiëntie met een IC50 van respectievelijk 1,5 μM en 2,2 μM voor CHO-ACAT1 en CHO-ACAT2. Consistent met ACAT-remming blokkeert deze verbinding de ACAT-afhankelijke processen in macrofagen, oxysterol-geïnduceerde apoptose en geacetyleerd-LDL-geïnduceerde schuimcelvorming. Het antagoniseert de remmende effecten van Cannabinoid Receptor-agonisten op zowel de samentrekkingen van de muisvas deferens als de adenylylcyclase-activiteit in rattenhersenvliezen op een concentratieafhankelijke manier. De verbinding vermindert de celgroei aanzienlijk en induceert celdood van menselijke colorectale kankercellen (DLD-1, CaCo-2 en SW620). Het is in staat om de celcyclusdistributie in alle geteste cellijnen te wijzigen. In het bijzonder produceert Rimonabant een G2/M-celcyclusarrest in DLD-1-cellen zonder apoptose of necrose te induceren.
Kinase Assay	Radioligand Bindingsanalyse
Kinase Assay	Menselijke CB1- en CB2-stabiel getransfecteerde HEK 293-cellen en celmembraan worden gezuiverd. 0,2-8 μg van de gezuiverde membraan wordt geïncubeerd met 0,75 nM [³H] CP55,940 en Rimonabant (SR141716) in de incubatiebuffer (50 mM Tris-HCl, 5 mM MgCl₂, 1 mM EDTA, 0,3% BSA, pH 7,4). De niet-specifieke binding wordt gedefinieerd in aanwezigheid van 1 μM CP55,940. De reacties worden anderhalf uur bij 30 °C in Multiscreen geïncubeerd. De reacties worden beëindigd door meervoudige filtratie en vier keer gewassen met ijskoude wasbuffer (50 mM Tris, pH 7,4, 0,25% BSA). De radioactiviteit gebonden aan de filters wordt gemeten door Topcount. De IC50 wordt bepaald als de concentratie van deze verbinding die nodig is om 50% van de binding van [³H] CP55,940 te remmen en berekend door niet-lineaire regressie.
In vivo	Rimonabant (SR141716) wordt intraperitoneaal of oraal toegediend en antagoniseert krachtig en dosisafhankelijk klassieke farmacologische en gedragsmatige effecten van Cannabinoid Receptor-agonisten. In het muismodel van azoxymethaan-geïnduceerde coloncarcinogenese verminderde het significant de vorming van aberrante crypten (ACF), die colorectale kanker voorafgaat. Deze verbinding (10 mg/kg via sondevoeding) wordt gedurende 2 weken aan 3 maanden oude mannelijke obese Zucker-ratten gevoerd als een model voor verminderde glucosetolerantie en gedurende 10 weken aan 6 maanden oude mannelijke obese Zucker-ratten als een model voor het metabool syndroom. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) en MCP-1 (monocyte chemotactic protein-1) serumniveaus zijn verhoogd bij obese versus magere Zucker-ratten en significant verlaagd door langdurige behandeling ermee, wat de gewichtstoename bij ratten met het metabool syndroom vertraagt. Neutrofielen en monocyten zijn significant verhoogd bij jonge en oude obese versus magere Zucker-ratten en verlaagd door deze verbinding. Bloedplaatjes-gebonden fibrinogeen is significant verhoogd bij obese versus magere Zucker-ratten van beide leeftijden, en wordt erdoor verminderd. Bloedplaatjes van obese ratten zijn gevoeliger voor trombine-geïnduceerde aggregatie en adhesie aan fibrinogeen, die beide worden afgezwakt door Rimonabant-therapie.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/18802648/ [2] https://pubmed.ncbi.nlm.nih.gov/20609360/ [3] https://pubmed.ncbi.nlm.nih.gov/8070571/ [4] https://pubmed.ncbi.nlm.nih.gov/19479993/ [5] https://pubmed.ncbi.nlm.nih.gov/18469848/ [6] https://pubmed.ncbi.nlm.nih.gov/17213845/ [7] https://pubmed.ncbi.nlm.nih.gov/30682372/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	CD44 / Lgr5 / CD133 / EpCAM β-catenin p-LRP6 / LRP6 / Lgr5		29354056
Immunofluorescence	β-catenin Lgr5		29354056

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT00750347	Completed	Pain	University Hospital Clermont-Ferrand	September 2008	Phase 1
NCT00656487	Completed	Cannabis Dependence\|Cannabis Withdrawal	The Scripps Research Institute\|National Institute on Drug Abuse (NIDA)	April 30 2008	Phase 2
NCT00546325	Completed	Diabetes Mellitus Type 2	Sanofi	October 2007	Phase 3
NCT00525681	Completed	Renal Transplantation	University of Oslo School of Pharmacy	September 2007	Phase 4
NCT00584389	Terminated	Obesity	University of Surrey\|European Foundation for the Study of Diabetes\|Royal Surrey County Hospital NHS Foundation Trust	July 2007	Phase 4
NCT01041170	Completed	Cannabis\|Dependence	National Institute on Drug Abuse (NIDA)\|National Institutes of Health Clinical Center (CC)	April 16 2006	Phase 1

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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