A soft-drug agonist of S1P1 (IC50 = 25.12 nM); selective for S1P1 over S1P2

CAY10739 – 5 mg

Brand:
Cayman
CAS:
2328109-05-1
Storage:
-20
UN-No:
Non-Hazardous - /

CAY10739 is a soft-drug agonist of the sphingosine-1-phosphate receptor 1 (S1P1; IC50 = 25.12 nM in a β-arrestin recruitment assay) that was designed to prevent systemic effects following topical application.{35828} It is selective for S1P1 over S1P2, S1P3, and S1P4 (IC50s = 1,000, >10,000, >10,000 nM, respectively, in a β-arrestin recruitment assay). In human S9 skin subcellular fractions, an ester group that protects an unstable phenol group is cleaved to release the active soft drug. The active soft drug and its nonenzymatically formed isomers are rapidly metabolized in isolated human hepatocytes.  

 

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SKU: 27837 - 5 mg Category:

Description

A soft-drug agonist of S1P1 (IC50 = 25.12 nM); selective for S1P1 over S1P2, S1P3, and S1P4 (IC50s = 1,000, >10,000, >10,000 nM, respectively); designed to be activated in the skin and rapidly metabolized to avoid systemic effects

Formal name: (2Z,5Z)-5-[[4-(acetyloxy)-3-methylphenyl]methylene]-3-(2-methylphenyl)-2-(propylimino)-4-thiazolidinone

Synonyms: 

Molecular weight: 408.5

CAS: 2328109-05-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Lipid Biochemistry|Sphingolipids

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