A potent S1P receptor antagonist (EC50s = 0.093

Etrasimod – 1 mg

Brand:
Cayman
CAS:
1206123-37-6
Storage:
-20
UN-No:
Non-Hazardous - /

Etrasimod is an orally bioavailable and potent antagonist of sphingosine-1-phosphate (S1P) receptors with EC50 values of 0.093, 0.44, 0.32, 0.34, and 0.32 nM for human, mouse, rat, dog, and monkey S1P1 receptors.{41302} It is selective for S1P1, S1P4, and S1P5 receptors with EC50 values of 6.1, >10,000, >10,000, 147, and 24.4 nM for S1P1-5, respectively, in a β-arrestin assay. Etrasimod (1 mg/kg, i.v.) decreases peripheral lymphocytes in mouse, rat, dog, and monkey (IC50s = 101, 51, 58, and 98 nM, respectively). It delays or prevents the onset and severity of murine experimental autoimmune encephalomyelitis (EAE) when administered at 0.3, 1, or 3 mg/kg. It also leads to lower EAE disease scores relative to vehicle when administered after disease onset and is efficacious in a rat model of collagen-induced arthritis.  

 

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Description

A potent S1P receptor antagonist (EC50s = 0.093, 0.44, 0.32, 0.34, and 0.32 nM for human, mouse, rat, dog, and monkey S1P1 receptors); selective for S1P1, S1P4, and S1P5 receptors (EC50 = 6.1, >10,000, >10,000, 147, and 24.4 nM for S1P1-5, respectively); decreases peripheral lymphocytes in mouse, rat, dog, and monkey (IC50s = 101, 51, 58, and 98 nM, respectively) when administered at a dose of 1 mg/kg, i.v.; delays or prevents the onset and severity of murine EAE at doses of 0.3, 1, or 3 mg/kg

Formal name: (3R)-7-[[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy]-1,2,3,4-tetrahydro-cyclopent[b]indole-3-acetic acid

Synonyms:  APD334

Molecular weight: 457.5

CAS: 1206123-37-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Lipid Biochemistry|Sphingolipids||Research Area|Neuroscience

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