ChemicalBook > CAS DataBase List > daprodustat

daprodustat

Product Name: 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
Formula Weight: 393.43
MOL File: 960539-70-2.mol

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daprodustat Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 19915
Product name: Daprodustat
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 19915
Product name: Daprodustat
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 19915
Product name: Daprodustat
Purity: ≥98%
Packaging: 10mg
Price: $261
Updated: 2024/03/01

Cayman Chemical

Product number: 19915
Product name: Daprodustat
Purity: ≥98%
Packaging: 25mg
Price: $533
Updated: 2024/03/01

TRC

Product number: D193368
Product name: Daprodustat
Packaging: 10mg
Price: $90
Updated: 2021/12/16

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daprodustat Chemical Properties,Usage,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

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daprodustat Suppliers

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View Lastest Price from daprodustat manufacturers

Anhui Dexinjia Biopharm Co., Ltd

Product: Daprodustat 960539-70-2
Price: US $100.00-2500.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 2MT per month
Release date: 2025-05-19

Wuhan Nutra Biotechnology Co.,Ltd

Product: Daprodustat 960539-70-2
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 98%
Supply Ability: 100kgs
Release date: 2021-05-24

Hangzhou Hyper Chemicals Limited

Product: Daprodustat 960539-70-2
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: EP/USP
Supply Ability: 1 ton
Release date: 2024-09-06

960539-70-2, daprodustatRelated Search:

N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide GSK-2126458 ABT 702 Dihydrochloride Danirixin GSK1940029 GSK 189254A GSK2110183 gsk2200150a 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide 4-Methoxy-N-(2,4,6-triMethylphenyl)benzenesulfonaMide, 97%

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

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