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W146(trifluoroacetate salt)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
W146(trifluoroacetate salt)图片
CAS NO:909725-62-8
包装与价格：
包装价格(元)
500μg电议
1mg电议
5mg电议
10mg电议

产品介绍
W146 (trifluoroacetate salt) 是 1-磷酸鞘氨醇受体 1 (S1PR1) 的选择性拮抗剂，EC50 值为 398 nM。
Cas No.909725-62-8
别名[(3R)-3-氨基-4-[(3-己基苯基)氨基]-4-氧代丁基]-膦酸单(三氟乙酸盐)
化学名[3R-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl]-phosphonic acid, mono(trifluoroacetate)
Canonical SMILESCCCCCCC1=CC=CC(NC([C@H](N)CCP(O)(O)=O)=O)=C1.FC(F)(C(O)=O)F
分子式C16H27N2O4P•CF3COOH
分子量456.4
溶解度0.1mg/mL in methanol
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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. 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 &#181M 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.

Reference:
[1]. Takuwa, Y., Takuwa, N., and Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. J. Biochem. 131(6), 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., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim. Biophys. Acta 1582(1-3), 72-80 (2002).
[4]. Sanna, M.G., Wang, S.K., Gonzalez-Cabrera, P.J., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nature Chemical Biology 2(8), 434-441 (2006).