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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-AUY954 hydrochloride
AUY954 hydrochloride

Chemical Structure : AUY954 hydrochloride

CAS No.: 820240-78-6

AUY954 hydrochloride

货号: PC-23526Not For Human Use, Lab Use Only.

AUY954 hydrochloride is a potent, selective sphingosine-1-phosphate (S1P1) receptor agonist with EC50 of 1.2 nM (hS1P1) and 0.9 nM (mS1P1) in γ-GTPS-binding assays, >280-fold selective over S1P2-5.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AUY954 hydrochloride is a potent, selective sphingosine-1-phosphate (S1P1) receptor agonist with EC50 of 1.2 nM (hS1P1) and 0.9 nM (mS1P1) in γ-GTPS-binding assays, >280-fold selective over S1P2-5.
AUY954 shows no appreciable binding affinity against a diverse panel of receptors and ion channels at 10 uM.
AUY954 increased Erk (tyrosine residue 204) and Akt phosphorylation (serine residue 473) levels with an EC50 of approximately 0.1 and 1 nM, respectively in S1P1 expressing CHO cells.
AUY954 induces a rapid, potent, and dose-dependent decrease in the number of peripheral lymphocytes in Lewis rats.
AUY954 is capable of prolonging the survival of cardiac allografts in a stringent rat transplantation model, in combination with RAD001 (Certican/Everolimus, an mTOR inhibitor).

物理化学性质&存储条件

分子量 491.95
分子式 C25H21ClF3NO2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(((2-(2-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)benzo[b]thiophen-5-yl)methyl)amino)propanoic acid hydrochloride

参考文献

1. Blé FX, et al. Br J Pharmacol. 2009 Nov;158(5):1295-301.

2. Pan S, et al. Chem Biol. 2006 Nov;13(11):1227-34.

3. Zhang ZY, et al. J Neuroimmunol. 2009 Nov 30;216(1-2):59-65.

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