AUY954 | S1P1 agonist | Probechem Biochemicals

Chemical Structure : AUY954

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AUY954 (AUY-954)

货号: PC-23525Not For Human Use, Lab Use Only.

AUY954 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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生物&药学活性

AUY954 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	455.50
分子式	C25H20F3NO2S
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

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.

AUY954 (AUY-954)

生物&药学活性

物理化学性质&存储条件

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AUY954 (AUY-954)

生物&药学活性

物理化学性质&存储条件

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