SAR247799 | S1P1 agonist | Probechem Biochemicals

Chemical Structure : SAR247799

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SAR247799 (SAR 247799)

货号: PC-72368Not For Human Use, Lab Use Only.

SAR247799 is a potent, selective G protein-biased S1P1 agonist with EC50 of 39 and 19 nM in β-arrestin and internalization assays, respectivey.

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生物&药学活性

SAR247799 is a potent, selective G protein-biased S1P1 agonist with EC50 of 39 and 19 nM in β-arrestin and internalization assays, respectivey.
SAR247799 preferentially activated the Gi pathway, induced a concentration-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt, EC50, 72.9 to 118 nM).
SAR247799 is inactive at S1P2, S1P3, and S1P5, and the EC50 value for S1P4 is >100-fold higher than that for S1P1 in inhibiting cAMP production.
SAR247799 induced phosphorylation of Ser1177 of endothelial nitric oxide synthase (eNOS) in a S1P1-dependent manner, indicating eNOS activation.
SAR247799 improved the microvascular hyperemic response without reducing lymphocyte numbers in a pig model of coronary endothelial damage.

物理化学性质&存储条件

分子量	425.825
分子式	C21H16ClN3O5
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	2-(4-(5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl)-2,6-dimethylphenoxy)acetic acid

参考文献

1. Bruno Poirier, et al. Sci Signal. 2020 Jun 2;13(634):eaax8050.

SAR247799 (SAR 247799)

生物&药学活性

物理化学性质&存储条件

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SAR247799 (SAR 247799)

生物&药学活性

物理化学性质&存储条件

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