An S1P1 receptor agonist (IC50 = 0.6 nM); selectively binds S1P1 over S1P2

CAY10734 – 1 mg

Brand:
Cayman
CAS:
635701-59-6
Storage:
-20
UN-No:
Non-Hazardous - /

CAY10734 is an agonist of sphingosine-1-phosphate receptor 1 (S1P1; IC50 = 0.6 nM).{13377} It selectively binds S1P1 over S1P2, S1P3, and S1P4 receptors (IC50s = >10,000, 12,000, and 70 nM, respectively) but does also bind S1P5 receptors (IC50 = 1 nM) in radioligand binding assays. CAY10734 reduces the number of peripheral blood lymphocytes in mice, rats, and dogs, with the maximal response achieved when administered at doses of 10, 0.5, and 0.5 mg/kg, respectively. It increases graft survival in a rat skin allograft model when administered at a dose of 5 mg/kg per day in combination with cyclosporin A (CsA; Item No. 12088).  

 

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SKU: 10007833 - 1 mg Category:

Description

An S1P1 receptor agonist (IC50 = 0.6 nM); selectively binds S1P1 over S1P2, S1P3, and S1P4 receptors (IC50s = >10,000, 12,000, and 70 nM, respectively) but does also bind S1P5 receptors (IC50 = 1 nM) in radioligand binding assays; reduces the number of peripheral blood lymphocytes in mice, rats, and dogs, with the maximal response achieved at 10, 0.5, and 0.5 mg/kg, respectively; increases graft survival in a rat skin allograft model at 5 mg/kg per day in combination with CsA

Formal name: 1-[[4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]-3-azetidinecarboxylic acid

Synonyms: 

Molecular weight: 391.5

CAS: 635701-59-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Immunosuppressants||Research Area|Lipid Biochemistry|Sphingolipids

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