A potent

W146 (trifluoroacetate salt) – 500 µg

Brand:
Cayman
CAS:
909725-62-8
Storage:
-20
UN-No:
Non-Hazardous - /

Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material).{14254} No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.  

 

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SKU: 10009109 - 500 µg Category:

Description

A potent, selective S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor with no activity at 10 µM at S1P2, S1P3, or S1P5 receptors; causes capillary leakage and inhibition of S1P1 agonist-induced lymphocyte sequestration in vivo

Formal name: [3R-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl]-phosphonic acid, mono(trifluoroacetate)

Synonyms: 

Molecular weight: 456.4

CAS: 909725-62-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Sphingolipids

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