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
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
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..…
N-Bromosuccinimide Price
- Product number
- 19915
- Product name
- Daprodustat
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 19915
- Product name
- Daprodustat
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 19915
- Product name
- Daprodustat
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $261
- Updated
- 2024/03/01
- Product number
- 19915
- Product name
- Daprodustat
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- D193368
- Product name
- Daprodustat
- Packaging
- 10mg
- Price
- $90
- Updated
- 2021/12/16
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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View Lastest Price from daprodustat manufacturers
- 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
- 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
- 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