Chemical Structure : AUY954 hydrochloride
CAS No.:
820240-78-6
AUY954 hydrochloride
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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491.95
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Formula
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C25H21ClF3NO2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(((2-(2-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)benzo[b]thiophen-5-yl)methyl)amino)propanoic acid hydrochloride
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References
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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