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Daprodustat

Names

[ CAS No. ]:
960539-70-2

[ Name ]:
Daprodustat

[Synonym ]:
N-[(1,3-Dicyclohexyl-2,4,6-trioxohexahydro-5-pyrimidinyl)carbonyl]glycine
(1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carbonyl)glycine
GSK-1278863
Glycine, N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]-
UNII:JVR38ZM64B
daprodustat
2-(1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carboxamido)acetic acid
GSK1278863

Biological Activity

[Description]:

Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase
Research Areas >> Cardiovascular Disease

[In Vitro]

GSK1278863 is an orally administered small-molecule PHI, and stimulates endogenous EPO synthesis and induce effective erythropoiesis[1]. GSK1278863 has been shown to increase erythropoietin levels, leading to increases in hemoglobin, hematocrit and red blood cell numbers[2].

[References]

[1]. Brigandi RA, et al. A Novel Hypoxia-Inducible Factor-Prolyl Hydroxylase Inhibitor (GSK1278863) for Anemia in CKD: A 28-Day, Phase 2A Randomized Trial. Am J Kidney Dis. 2016 Jun;67(6):861-71

[2]. Hara K, et al. Pharmacokinetics, pharmacodynamics and safety of single, oral doses of GSK1278863, a novel HIF-prolyl hydroxylase inhibitor, in healthy Japanese and Caucasian subjects. Drug Metab Pharmacokinet. 2015 Dec;30(6):410-8


[Related Small Molecules]

Dimethyloxalylglycine | PT-2385 | FG-4592 | PX-478 2HCl | BAY 87-2243 | Vadadustat | Oltipraz | Chlorogenic acid | LW 6 | Molidustat | IOX2 | Paeoniflorin | KC7F2 | oroxylin A | JNJ-42041935

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C19H27N3O6

[ Molecular Weight ]:
393.434

[ Exact Mass ]:
393.189972

[ PSA ]:
124.09000

[ LogP ]:
0.86

[ Appearance of Characters ]:
white solid

[ Index of Refraction ]:
1.580

[ Storage condition ]:
-20℃


Related Compounds