ChemicalBook >> CAS DataBase List >>daprodustat

daprodustat

CAS No.
960539-70-2
Chemical Name:
daprodustat
Synonyms
CS-1541;Dapstra;Dapusi Ta;GSK1278863;Daprodustat;GSK 1278863 NEW;GSK1278863, >98%;Daprodustat, >98%;13C12]-Daprodustat;GSK1278863,daprodustat
CBNumber:
CB63038532
Molecular Formula:
C19H27N3O6
Molecular Weight:
393.43
MDL Number:
MFCD29924726
MOL File:
960539-70-2.mol
Last updated:2025-07-04 15:06:11

daprodustat Properties

Melting point 237-241oC
Density 1.359±0.06 g/cm3(Predicted)
storage temp. Refrigerator
solubility Chloroform (Slightly), DMSO (Slightly)
pka 3.44±0.10(Predicted)
form Solid
color White to Off-White
InChI InChI=1S/C19H27N3O6/c23-14(24)11-20-16(25)15-17(26)21(12-7-3-1-4-8-12)19(28)22(18(15)27)13-9-5-2-6-10-13/h12-13,15H,1-11H2,(H,20,25)(H,23,24)
InChIKey RUEYEZADQJCKGV-UHFFFAOYSA-N
SMILES C(O)(=O)CNC(C1C(=O)N(C2CCCCC2)C(=O)N(C2CCCCC2)C1=O)=O
FDA UNII JVR38ZM64B

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319
Precautionary statements  P501-P270-P264-P280-P337+P313-P305+P351+P338-P302+P352-P332+P313-P362-P301+P310+P330-P405

daprodustat price More Price(24)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 19915 Daprodustat ≥98% 960539-70-2 1mg $32 2024-03-01 Buy
Cayman Chemical 19915 Daprodustat ≥98% 960539-70-2 5mg $139 2024-03-01 Buy
Cayman Chemical 19915 Daprodustat ≥98% 960539-70-2 10mg $261 2024-03-01 Buy
Cayman Chemical 19915 Daprodustat ≥98% 960539-70-2 25mg $533 2024-03-01 Buy
TRC D193368 Daprodustat 960539-70-2 10mg $90 2021-12-16 Buy
Product number Packaging Price Buy
19915 1mg $32 Buy
19915 5mg $139 Buy
19915 10mg $261 Buy
19915 25mg $533 Buy
D193368 10mg $90 Buy

daprodustat Chemical Properties,Uses,Production

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.

Mechanism of action

Daprodustat inhibits HIF-PH and reduces the degradation of HIF-α, thereby increasing the production of endogenous erythropoietin (EPO) and alleviating anemia symptoms.

Synthesis

Daprodustat can be prepared by the reaction of DCC (dicyclohexylcarbodiimide) and malonic acid (59). The cyclic urea 60 was generated with a yield of 72%. This step creatively used the classic coupling reagent DCC as a urea synthon and reacted in a modified Biginelli reaction. The cyclic urea 60 was placed under alkaline conditions and reacted in the presence of ethylisocyanoacetate to obtain the penultimate intermediate 61. The penultimate intermediate 61 was subjected to a saponification reaction to finally obtain daprodustat (IX) with a yield of 78%.
daprodustat synthesis route

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.

daprodustat Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 195)Suppliers
Supplier Tel Email Country ProdList Advantage
Shaanxi Dideu Medichem Co. Ltd
+86-29-81148696 +86-17392712697 1022@dideu.com China 3995 58
Hangzhou Hyper Chemicals Limited
+86-0086-57187702781 +8613675893055 info@hyper-chem.com China 295 58
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 33024 60
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29852 58
Anhui Dexinjia Biopharm Co., Ltd
+86-531-82375818 +86-15064153060 sales01@jndxj.com China 301 58
Shochem(Shanghai) Co.,Ltd
86-21-50800795 info@shochem.com CHINA 288 58
Wuhan Nutra Biotechnology Co.,Ltd
+8617786394783 nutrabiotech@outlook.com China 300 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 sales@sarms4muscle.com China 10473 58
Guangzhou TongYi biochemistry technology Co.,LTD
+8613073028829 mack@tongyon.com China 2994 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58

Related articles

  • Synthesis of Daprodustat
  • Daprodustat is synthesised using malonic acid as a raw material by Biginelli reaction, saponification and other reactions.
  • Dec 21,2023

View Lastest Price from daprodustat manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Daprodustat pictures 2025-09-23 Daprodustat
960539-70-2
US $100.00-2500.00 / KG 1KG 99% 2MT per month Anhui Dexinjia Biopharm Co., Ltd
Daprodustat pictures 2024-11-01 Daprodustat
960539-70-2
US $0.00-0.00 / g 1g 98% 100kgs Wuhan Nutra Biotechnology Co.,Ltd
Daprodustat pictures 2024-11-01 Daprodustat
960539-70-2
US $0.00-0.00 / KG 1KG EP/USP 1 ton Hangzhou Hyper Chemicals Limited
  • Daprodustat pictures
  • Daprodustat
    960539-70-2
  • US $100.00-2500.00 / KG
  • 99%
  • Anhui Dexinjia Biopharm Co., Ltd
  • Daprodustat pictures
  • Daprodustat
    960539-70-2
  • US $0.00-0.00 / g
  • 98%
  • Wuhan Nutra Biotechnology Co.,Ltd
  • Daprodustat pictures
  • Daprodustat
    960539-70-2
  • US $0.00-0.00 / KG
  • EP/USP
  • Hangzhou Hyper Chemicals Limited
daprodustat,GSK1278863 GSK1278863 Daprodustat 2-(1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carboxamido)acetic acid N-[(1,3-Dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]glycine GSK1278863; GSK 1278863; GSK-1278863; DAPRODUSTAT 2-[(1,3-dicyclohexyl-2,4,6-trioxo-1,3-diazinane-5-carbonyl)amino]acetic acid GSK1278863,daprodustat CS-1541 Daprodustat, >98% GSK1278863, >98% (1,3-dicyclohexyl-2,4,6-trioxohexahydropyrimidine-5-carbonyl)glycine GSK 1278863 NEW Glycine, N-[(1,3-dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]- Daprodustat Impurity 3 13C12]-Daprodustat Dapstra Dapusi Ta N-[(1,2-Dicyclohexylhexahydro-2,4,6-trioxo-5-pyrimidinyl)carbonyl]glycine 1,3-dicyclohexyl-1,3,6-triazonane-2,4,7,9-tetraone 960539-70-2 API