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KI1111W1460.5 mg$200
W1461 mg$384

Chemical Characteristic

Product NameW146
CAS No.909725-61-7
Molecular Weight 342.37
FormulaC16H27N2O4P
Chemical Name[(3R)-3-amino-4-[(3-hexylphenyl)ami閳ュ獧o]-4-oxobutyl]-phosphonic acid
SmilesC(C[C@@H](C(=O)Nc1cc(ccc1)CCCCCC)N)P(=O)(O)O
Chemical Structure

Biological activities

W146 is a huaman type 1 sphingosine-1-phosphate (S1P1) receptor antagonist. The IC50 of W146 is 0.8 µM against S1P1 receptor. W146 is equipotent on mouse and human S1P1 receptors.[1] W146 dose-dependently blocks the S1P1 receptor. W146 decreases the number of CD4+, CD8+ and CD19+ cells in blood.[1] W146 inhibits S1P1 receptor with a Ki of 18 nM.[2] W146 induces lymphopenia in blood and a concomitant increase of CD4+ and CD8+ T cells in lymph nodes.[3] W146 inhibits CYM-5442-mediated p42/p44 MAPK phosphorylation.[4] W146 significantly gives rise to short lasting lymphopenia in mice. In addition, W146 increases the number of total blood lymphocytes by 48% in W146-treated mice compared to vehicle-treated animals 4 hours after dosing. W146 causes lung edema concomitant to lymphopenia.[1] W146 dose-dependent blocks the development of S1P induced thermal-hyperalgesia in rats.[5]

Protocols

In vivo W146 is dissolved in 20% DMSO in saline.[5]

References

[1] Tarras?n G, et al. The sphingosine-1-phosphate receptor-1 antagonist, W146, causes early and short-lasting peripheral blood lymphopenia in mice. Int Immunopharmacol. 2011, 11(11): 1773-1779.
[2] Sanna MG, et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2006, 2(8): 434-441.
[3] Godessart N et al. The S1P1 receptor antagonist W146 induces lymphopenia in mice. Demonstration that functional antagonism of S1P1 is the mechanism of lymphopenia evoked by fingolimod-like compounds. J Immunol. 2010, 184: 140.15.
[4] Gonzalez-Cabrera PJ, et al. Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions. Mol Pharmacol. 2008??74(5): 1308-1318.
[5] Doyle T, et al. Role for peroxynitrite in sphingosine-1-phosphate-induced hyperalgesia in rats. Pain. 2011, 152(3): 643-648.

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