Name: Resiquimod (R-848)
Brand: Selleck Chemicals
SKU: S8133
Rating: 5 (19 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.98%

99.98

Dianas relacionadas	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Otros TLR Inhibidores	FSL-1 Resatorvid (TAK-242) TLR2-IN-C29 Lipopolysaccharides (LPS) Motolimod CU-CPT22 TLR4-IN-C34 Vesatolimod (GS-9620) E6446 Dihydrochloride E6446

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
PBMC	Function assay	30 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 30 nM after 18 hrs by ELISA, Activity=0.00125μM.	20232824
PBMC	Function assay	10 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 10 nM after 18 hrs by ELISA, Activity<0.00125μM.	20232824
PBMC	Function assay	100 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 100 nM after 18 hrs by ELISA, Activity=0.00561μM.	20232824
PBMC	Function assay	300 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 300 nM after 18 hrs by ELISA, Activity=0.00726μM.	20232824
PBMC	Function assay	1000 nM	18 hrs	Induction of type 1 IFN secretion in human PBMC at 1000 nM after 18 hrs by ELISA, Activity=0.00775μM.	20232824
Huh7	Antiviral assay		48 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced mixed donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.024μM.	17548497
Huh7	Antiviral assay		48 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 48 hrs with drug-induced single donor human PBMC supernatants assessed as viral levels by luciferase assay, EC50=0.0265μM.	17548497
PBMC	Function assay		24 hrs	Induction of IFNalpha2a level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=0.1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of IL1-beta level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of IL6 level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
PBMC	Function assay		24 hrs	Toxic induction of TNFalpha level in human PBMC assessed as drug level causing maximal cytokine induction after 24 hrs relative to control, Activity=1μM.	17548497
HEK293	Function assay		6 hrs	Agonist activity at human TLR7 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.1μM.	30143425
HEK293	Function assay			Agonist activity at human TLR7 expressed in HEK293 cells coexpressing pNiFty2-SEAP reporter by reporter gene assay, EC50=0.2601μM.	20232824
HEK293	Function assay		6 hrs	Agonist activity at human TLR8 expressed in HEK293 cells after 6 hrs by NFkappaB-luciferase reporter gene assay, MEC=0.3μM.	30143425
HEK	Function assay		8 to 12 hrs	Agonist activity at human TLR7 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=1.34μM.	29152046
HEK	Function assay		24 hrs	Agonist activity at human TLR7 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=1.4μM.	22837811
HEK293	Function assay		24 hrs	Agonist activity at human TLR-7 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=1.5μM.	24383475
HEK293	Function assay		6 hrs	Agonist activity at human TLR8 expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene assay, EC50=4μM.	27270029
HEK293	Function assay		24 hrs	Agonist activity at human TLR-8 expressed in HEK293 cells after 24 hrs by SEAP reporter gene assay, EC50=4.5μM.	24383475
HEK	Function assay		8 to 12 hrs	Agonist activity at human TLR8 expressed in HEK cells after 8 to 12 hrs by NFkappaB/SEAP reporter gene assay, EC50=6.13μM.	29152046
HEK	Function assay		24 hrs	Agonist activity at human TLR8 transfected in HEK cells assessed as NFkappaB induction after 24 hrs by specific secreted alkaline phosphatase gene assay, EC50=6.4μM.	22837811
PBMC	Function assay		24 hrs	Increase in IFNalpha level in human PBMC after 24 hrs relative to control	17548497
PBMC	Function assay		24 hrs	Increase in 2',5'-oligoadenylate synthase level in human PBMC after 24 hrs relative to control	17548497
PBMC	Toxicity assay		24 hrs	Toxicity assessed as increase in IL6 level in human PBMC after 24 hrs relative to control	17548497
Huh7	Antiviral assay		24 hrs	Antiviral activity against HCV infected human Huh7 replicon cells treated for 24 hrs with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay	17548497
Huh7	Antiviral assay			Antiviral activity against HCV infected human Huh7 replicon cells treated with drug-induced human PBMC supernatants assessed as viral levels by luciferase assay	17548497
PBMC	Function assay	22.5 uM	24 hrs	Agonist activity at TLR7/TLR8 in human PBMC assessed as induction of TNF-alpha production at 22.5 uM after 24 hrs by flow cytometric analysis	24383475
PBMC	Immunomodulatory assay	16 uM	24 hrs	Immunomodulatory activity in human PBMC assessed as induction of IL-6 secretion at 16 uM after 24 hrs by ELISA	28254484
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD86 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of MHC class-2 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	1 uM	48 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as upregulation of CD40 at 1 uM after 48 hrs by flow cytometry	19299126
BMD	Function assay	5 uM	24 hrs	Induction of TLR7 receptor-mediated C57BL/6 mouse BMD cells activation assessed as IL12 production at 5 uM after 24 hrs by ELISA	19299126
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	314.38	Fórmula	C₁₇H₂₂N₄O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	144875-48-9	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	S28463			Smiles	CCOCC1=NC2=C(N1CC(C)(C)O)C3=CC=CC=C3N=C2N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 62 mg/mL (197.21 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 51 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	3.150mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL 63 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	TLR7 TLR8
In vitro	Resiquimod (R-848) activa las células inmunitarias e induce la proliferación de esplenocitos de tipo salvaje a través de la vía de señalización dependiente del receptor tipo Toll 7 (TLR7)-MyD88. Este compuesto también modula las células dendríticas para aumentar las respuestas de las células T específicas del citomegalovirus y del VIH-1. Induce la diferenciación de células supresoras derivadas de mieloides en macrófagos y células dendríticas, y puede mejorar la inmunoterapia contra el cáncer al reducir las MDSC inmunosupresoras.
In vivo	En ratones de tipo salvaje, Resiquimod (R-848) (50 nmol, i.p.) induce un aumento de las concentraciones séricas de IFN-alpha, TNF-alpha e IL-12, mientras que ni los ratones deficientes en TLR7 ni los ratones deficientes en MyD88 muestran un aumento de estas citocinas. En un modelo murino de asma alérgica, este compuesto (i.n., 20 μg/ratón) reduce la reactividad e inflamación de las vías respiratorias inducidas por alérgenos mediante la reducción de la señalización de Nrf2.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/11812998/ [2] https://pubmed.ncbi.nlm.nih.gov/14530357/ [3] https://pubmed.ncbi.nlm.nih.gov/24748512/ [4] https://pubmed.ncbi.nlm.nih.gov/26851512/ [5] https://pubmed.ncbi.nlm.nih.gov/25475963/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06021002	Recruiting	Innate Inflammatory Response\|Asthma\|Nasal Allergy	Cambridge University Hospitals NHS Foundation Trust	August 9 2022	Not Applicable
NCT04127864	Active not recruiting	Colorectal Cancer\|Surgery	University of Copenhagen\|Zealand University Hospital	October 14 2019	--
NCT02688478	Unknown status	Allergies	University of British Columbia	February 2 2017	Not Applicable
NCT00960752	Completed	Melanoma	M.D. Anderson Cancer Center	May 20 2010	Phase 2

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Resiquimod (R-848) agonista TLR7/8

Estructura química

Peso molecular: 314.38

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

Resiquimod (R-848) agonista TLR7/8

Estructura química

Peso molecular: 314.38

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)