Daprodustat (GSK1278863) | HIF-PHD inhibitor | Probechem Biochemicals

Chemical Structure : Daprodustat

CAS No.: 960539-70-2

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Daprodustat (GSK-1278863, GSK1278863)

货号: PC-45387Not For Human Use, Lab Use Only.

Daprodustat (GSK1278863) is a potent, orally active HIF-prolyl hydroxylase (PHD) inhibitor with IC50 of 3.5, 22.2 and 2.2 nM for PHD1, PHD2 and PHD3, respectively.

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5 mg	￥680	In stock
10 mg	￥980	In stock
25 mg	￥1580	In stock
50 mg	￥2480	In stock
100 mg		Get quote

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生物&药学活性

Daprodustat (GSK1278863) is a potent, orally active HIF-prolyl hydroxylase (PHD) inhibitor with IC50 of 3.5, 22.2 and 2.2 nM for PHD1, PHD2 and PHD3, respectively.
Daprodustat (GSK1278863) displays high selectivity over α-KG-dependent iron dioxygenases FIH and CP4H (IC50>9800 nM).

Daprodustat (GSK1278863) stimulate endogenous EPO synthesis and induces effective erythropoiesis by non-EPO effects.

Daprodustat (GSK1278863) shows potential for the treatment of anemia associated with chronic kidney disease.

物理化学性质&存储条件

分子量	393.4342
分子式	C19H27N3O6
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	DMSO: < 6.8 mg/mL
Chemical Name/SMILES	Glycine, N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]-

参考文献

1. Brigandi RA, et al. Am J Kidney Dis. 2016 Jun;67(6):861-71.

2. Hara K, et al. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8.

3. Johnson BM, et al. Clin Pharmacol Drug Dev. 2014 Mar;3(2):109-17.
4. Ariazi JL, et al. J Pharmacol Exp Ther. 2017 Dec;363(3):336-347.

Daprodustat (GSK-1278863, GSK1278863)

生物&药学活性

物理化学性质&存储条件

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Daprodustat (GSK-1278863, GSK1278863)

生物&药学活性

物理化学性质&存储条件

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