GSK1120360A (GSK360A)

Chemical Structure : GSK1120360A

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货号: PC-49790Not For Human Use, Lab Use Only.

GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.

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生物&药学活性

GSK1120360A (GSK360A) is a potent, specific and orally active inhibitor of HIF PHD enzyme with pIC50 of 8.0/7.0/6.9 for PHD1/2/3, respectively.
GSK360A acts by competing with the a-ketoglurtarate site and has little or no activity on inhibiting HIF-1 asparaginyl hydroxylase (FIH-1) or collagen 4-prolyl hydroxylase (pIC50 =5.0 and 5.7, respectively).
GSK360A increased secreted EPO protein level by 50% at 3 uM and vascular endothelial growth factor protein level by 50% at 1 uM, respectively, in Hep3B cells.
GSK360A exerts systemic and local effects by stabilizing HIF-1 alpha signaling and improves long-term ventricular function, remodeling, and vascularity in a model of established ventricular dysfunction.
GSK360A enhances rotator cuff regeneration following a chronic tear.

物理化学性质&存储条件

分子量	348.33
分子式	C17H17FN2O5
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	N-{[1-(2-cyclopropylethyl)-6-fluoro-4-hydroxy-2-oxo-1, 2-dihydro-3-quinolinyl] carbonyl} glycine

参考文献

1. Weike Bao, et al. J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55.

2. J P Gumucio, et al. Bone Joint Res. 2017 Jan;6(1):57-65.