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
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) | ![]() 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 |
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%.
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
Supplier | Tel | 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 | |
---|---|---|---|---|---|---|---|---|
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2025-09-23 | Daprodustat
960539-70-2
|
US $100.00-2500.00 / KG | 1KG | 99% | 2MT per month | Anhui Dexinjia Biopharm Co., Ltd | |
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2024-11-01 | Daprodustat
960539-70-2
|
US $0.00-0.00 / g | 1g | 98% | 100kgs | Wuhan Nutra Biotechnology Co.,Ltd | |
![]() |
2024-11-01 | Daprodustat
960539-70-2
|
US $0.00-0.00 / KG | 1KG | EP/USP | 1 ton | Hangzhou Hyper Chemicals Limited |
-
- Daprodustat
960539-70-2
- US $100.00-2500.00 / KG
- 99%
- Anhui Dexinjia Biopharm Co., Ltd
-
- Daprodustat
960539-70-2
- US $0.00-0.00 / g
- 98%
- Wuhan Nutra Biotechnology Co.,Ltd
-
- Daprodustat
960539-70-2
- US $0.00-0.00 / KG
- EP/USP
- Hangzhou Hyper Chemicals Limited