960539-70-2 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 960539-70-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,6,0,5,3 and 9 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 960539-70:
(8*9)+(7*6)+(6*0)+(5*5)+(4*3)+(3*9)+(2*7)+(1*0)=192
192 % 10 = 2
So 960539-70-2 is a valid CAS Registry Number.
960539-70-2Relevant articles and documents
Substituted pyrimidinetrione compound, composition containing same and application of substituted pyrimidinetrione compound
-
Paragraph 0077; 0080; 0085; 0086, (2018/11/22)
The invention provides a substituted pyrimidinetrione compound, a composition containing the same and application of the substituted pyrimidinetrione compound. The invention discloses the pyrimidinetrione compound as shown in formula (I) or the crystal form, pharmaceutically acceptable salt, prodrug, stereisomer, hydrate or solvent compound thereof. The pyrimidinetrione compound and the composition containing the same can be used for regulating hypoxia-inducible factors (HIF) and/or erythropoietin (EPO) and can be used for preparing medicine for regulating and controlling human body anemia.
