10009109  W146 (trifluoroacetate salt)



• See below for pricing and ordering
• See more Receptor Antagonist; Immunology

For active pharmaceutical ingredients (APIs) related to W146 (trifluoroacetate salt), see Cayman Pharma

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.1,2,3 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-8.1,2 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).4 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.
1  Takuwa, Y., Takuwa, N., Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. J Biochem 131 767-771 (2002).
2  Ishii, I., Fukushima, N., Ye, X., et al. Lysophospholipid receptors: Signaling and biology. Annu Rev Biochem 73 321-354 (2004).
3  Kluk, M.J., Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim Biophys Acta 1582 72-80 (2002).
4  Sanna, M.G., Wang, S., Gonzalez-Cabrera, P.J., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol 2(8) 434-441 (2006).

Download Product Insert 129 Kb PDF
Download Material Safety Data Sheet (MSDS) 15 Kb PDF

Pricing Information

Prices listed here are the Manufacturer's Suggested European Retail Price. The actual prices quoted by each individual distributor may vary. Please visit the Global Buyer's Guide on the Cayman Chemical (world) website to locate a distributor in your region.

This product is also available to buy in bulk quantities. Please contact us for a quote or to purchase.

Cayman strives to be a reliable biochemical reagent vendor by providing the best possible products and services. To ask for assistance with one of our products please contact our Technical Help staff.

Warning This product is not for human or veterinary use.

Item total €0.00
Shopping cart total €0.00
Size Price Quantity
500 µg €75.00
1 mg €142.00
5 mg €596.00
10 mg €1,042.00
Pricing updated 2010-08-01.
Prices are subject to change without notice.