Name: Prostaglandin E2 (PGE2)
Brand: Selleck Chemicals
SKU: S3003
Rating: 5 (29 reviews)

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Control de calidad

Lote: Pureza: >97%

Citado en Nature Medicine por su calidad de primer nivel
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SDS

Citado en Nature Medicine por su calidad de primer nivel
COA
Ficha técnica
SDS

Citado en Nature Medicine por su calidad de primer nivel
COA
NMR
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SDS

Citado en Nature Medicine por su calidad de primer nivel
COA
NMR
Ficha técnica
SDS

Citado en Nature Medicine por su calidad de primer nivel
COA
NMR
Ficha técnica
SDS

97

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Otros PGES Inhibidores	Yakuchinone A

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
HeLa	Function assay			TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, Km = 0.094 μM.	7754369
HeLa	Function assay			TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, K1/2 = 0.1 μM.	8787677
S2	Function assay			TP_TRANSPORTER: uptake in OCT2-expressing S2 cells, Km = 0.0289 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT4-expressing S2 cells, Km = 0.154 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT3-expressing S2 cells, Km = 0.345 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OCT1-expressing S2 cells, Km = 0.657 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT2-expressing S2 cells, Km = 0.713 μM.	11907186
S2	Function assay			TP_TRANSPORTER: uptake in OAT1-expressing S2 cells, Km = 0.97 μM.	11907186
HEK293	Function assay			Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cells, IC50 = 0.0007 μM.	12643927
HEK293	Function assay			EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor, EC50 = 0.003 μM.	12643927
Sf9	Function assay			TP_TRANSPORTER: uptake (vesicle) in membrane vesicles from MRP4-expressing Sf9 cells, Km = 3.4 μM.	12835412
HEK293	Function assay			Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells, Ki = 0.00033 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells, Ki = 0.00079 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells, Ki = 0.0049 μM.	17531488
HEK293	Function assay			Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells, Ki = 0.0091 μM.	17531488
HEK293	Function assay			Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0002 μM.	19250823
HEK293	Function assay			Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0007 μM.	19250823
HEK293	Function assay			Inhibition of rat EP4 receptor expressed in HEK293 cells, IC50 = 0.0021 μM.	19250823
HEK293	Function assay			Inhibition of rat EP2 receptor expressed in HEK293 cells, IC50 = 0.0052 μM.	19250823
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0031 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.005 μM.	22119471
CHO	Function assay		20 mins	Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting, Ki = 0.006 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.022 μM.	22119471
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.0031 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.005 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.006 μM.	22386979
CHO	Function assay		60 mins	Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.022 μM.	22386979
CHEM1	Function assay		2 hrs	Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, Ki = 0.00045 μM.	23403082
CHEM1	Function assay		2 hrs	Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, IC50 = 0.0011 μM.	23403082
CHO	Function assay	100 nM		Activity at recombinant EP1 receptor (unknown origin) expressed in CHO cells co-expressing Gq protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay	100 nM		Activity at recombinant EP4 receptor (unknown origin) expressed in CHO cells co-expressing Gs protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay	100 nM		Activity at recombinant EP3 receptor (unknown origin) expressed in CHO cells co-expressing Gi protein at 100 nM by electrical cell substrate impedance sensing system	25701254
CHO	Function assay		30 mins	Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0019 μM.	26985320
CHO	Function assay			Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0025 μM.	26985320
CHO	Function assay			Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0037 μM.	26985320
CHO	Function assay		30 mins	Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0075 μM.	26985320
Chem1	Function assay			Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.25 μM.	26985320
HEK293	Function assay		90 mins	Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay, EC50 = 0.346 μM.	26985320
CHO	Function assay		30 mins	Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.347 μM.	26985320
HEK293	Function assay			Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells, IC50 = 0.0026 μM.	26988801
HEK293	Function assay		120 mins	Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.00055 μM.	27876250
HEK293	Function assay		120 mins	Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.0026 μM.	27876250
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Información química, almacenamiento y estabilidad

Peso molecular	352.47	Fórmula	C₂₀H₃₂O₅	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	363-24-6	Descargar SDF		Almacenamiento de soluciones madre	Las soluciones son inestables. Preparar frescas o comprar tamaños pequeños preenvasados. Reenvasar al recibirlas.
Sinónimos	Dinoprostone			Smiles	CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O

Solubilidad

In vitro
Lote:

DMSO : 70 mg/mL (198.59 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 70 mg/mL

Water : 2.5 mg/mL

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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.	3.500mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 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 clarify; 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.
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.
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

In vitro	Prostaglandin E2 actúa a través de los receptores EP4 en los osteoclastos durante la progresión de la OA y el dolor relacionado con la OA.
In vivo	Prostaglandin E2 (0,3 μg/k, i.p.) reduce significativamente el número de macrófagos peritoneales que sufren fagocitosis de las microesferas de metacrilato en ratas.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/6804558/

Información del ensayo clínico

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT06129604	Recruiting	Colorectal Carcinoma (CRC)\|Endometrial Carcinoma (EC)	University of Oklahoma	April 3 2024	Phase 2
NCT06307678	Completed	Periapical; Infection	Ataturk University	July 7 2023	Not Applicable
NCT06190132	Completed	Uremic Pruritus in Hemodialysis Patients	Ain Shams University	April 1 2023	Not Applicable

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Instrucciones de manipulación

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Prostaglandin E2 (PGE2) Agonista del Prostaglandin Receptor

Estructura química

Peso molecular: 352.47