| Identification | Back Directory | [Name]
daprodustat,GSK1278863 | [CAS]
960539-70-2 | [Synonyms]
CS-1541
GSK1278863
Daprodustat
GSK 1278863 NEW
GSK1278863, >98%
Daprodustat, >98%
daprodustat,GSK1278863
GSK1278863,daprodustat
Daprodustat Impurity 3
GSK1278863; GSK 1278863; GSK-1278863; DAPRODUSTAT
(1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carbonyl)glycine
N-[(1,3-Dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]glycine
2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinane-5-carbonyl)amino]acetic acid
Glycine, N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]-
2-(1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carboxamido)acetic acid | [EINECS(EC#)]
691-659-9 | [Molecular Formula]
C19H27N3O6 | [MDL Number]
MFCD29924726 | [MOL File]
960539-70-2.mol | [Molecular Weight]
393.43 |
| Chemical Properties | Back Directory | [Melting point ]
237-241oC | [density ]
1.359±0.06 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
Chloroform (Slightly), DMSO (Slightly) | [form ]
Solid | [pka]
3.44±0.10(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
Daprodustat is a novel HIF (Hypoxia inducible factor)-prolyl hydroxylase inhibitor. | [Biological Activity]
daprodustat (gsk1278863) is a hif-prolyl hydroxylase inhibitor.hypoxia stimulates erythropoietin (epo) release through accumulation of hypoxia-inducible factor 1α (hif-1α), resulting in an increase of erythrocyte production by the bone marrow. hif-prolyl hydroxylase inhibitors have been used to selectively activate the phd-signaling pathway, leading to the stabilization of hifα subunits, which can affect the transcription of hif-responsive genes. | [in vitro]
in-vitro biotransformation data indicated that gsk1278863 was primarily metabolized by cyp2c8 [1]. | [References]
[1] hara k,takahashi n,wakamatsu a,caltabiano s. 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.
[2] brigandi ra,johnson b,oei c,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. |
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