A potent S1P1 receptor agonist (IC50s = 6

Ponesimod – 1 mg

Brand:
Cayman
CAS:
854107-55-4
Storage:
-20
UN-No:
Non-Hazardous - /

Ponesimod is a potent agonist of sphingosine-1-phosphate receptor 1 (S1P1/EDG-1; IC50s = 6, >10,000, 2,068, 1,956, and 142 nM for S1P1-S1P5, respectively, in a radioligand binding assay).{38368} It selectively activates S1P1 in a GTPγS assay (EC50s = 5.7, >10,000, 105, 1,108, and 59.1 nM, for S1P1-S1P5, respectively). Ponesimod (3-100 mg/kg) reduces the number of circulating lymphocytes in rats in a dose-dependent manner. It reduces edema, protein extravasation, neutrophil activity, and skin levels of the proinflammatory cytokines IL-1β, IL-6, IFN-γ, and TNF-α in a mouse model of delayed-type hypersensitivity at a dose of 30 mg/kg.{38369} Ponesimod (30 mg/kg) also prevents footpad swelling in a rat model of adjuvant-induced arthritis.  

 

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Description

A potent S1P1 receptor agonist (IC50s = 6, >10,000, 2,068, 1,956, and 142 nM for S1P1-S1P5, respectively, in a radioligand binding assay); selectively activates S1P1 in a GTPγS assay (EC50s = 5.7, >10,000, 105, 1,108, 59.1 nM, for S1P1-S1P5, respectively); reduces the number of circulating lymphocytes in rats in a dose-dependent manner; reduces edema, protein extravasation, neutrophil activity, and skin levels of the proinflammatory cytokines IL-1β, IL-6, IFN-γ, and TNF-α in a mouse model of delayed-type hypersensitivity; prevents footpad swelling in a rat model of adjuvant-induced arthritis ,

Formal name: (2Z)-5Z-[[3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl]methylene]-3-(2-methylphenyl)-2-(propylimino)-4-thiazolidinone

Synonyms: 

Molecular weight: 461

CAS: 854107-55-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Innate Immunity

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