Vadadustat
- Product Name
- Vadadustat
- CAS No.
- 1000025-07-9
- Chemical Name
- Vadadustat
- Synonyms
- CS-2486;AKB-6548;Valdesta;PG1016548;PG-1016548;PG 1016548;Vadadustat;Vardorestat;Vadadustat 13C6;PG-1016548;AKB-6548
- CBNumber
- CB73147387
- Molecular Formula
- C14H11ClN2O4
- Formula Weight
- 306.7
- MOL File
- 1000025-07-9.mol
Vadadustat Property
- Melting point:
- 172-174°C
- Boiling point:
- 674.6±55.0 °C(Predicted)
- Density
- 1.461±0.06 g/cm3(Predicted)
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 4.09±0.40(Predicted)
- form
- Solid
- color
- Pale Beige to Light Beige
- Stability:
- Hygroscopic
- InChI
- InChI=1S/C14H11ClN2O4/c15-10-3-1-2-8(4-10)9-5-11(18)13(16-6-9)14(21)17-7-12(19)20/h1-6,18H,7H2,(H,17,21)(H,19,20)
- InChIKey
- JGRXMPYUTJLTKT-UHFFFAOYSA-N
- SMILES
- C(O)(=O)CNC(C1=NC=C(C2=CC=CC(Cl)=C2)C=C1O)=O
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H373May cause damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P314Get medical advice/attention if you feel unwell.
P330Rinse mouth.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 15295
- Product name
- Vadadustat
- Packaging
- 5mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 15295
- Product name
- Vadadustat
- Packaging
- 10mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 15295
- Product name
- Vadadustat
- Packaging
- 25mg
- Price
- $239
- Updated
- 2024/03/01
- Product number
- 15295
- Product name
- Vadadustat
- Packaging
- 50mg
- Price
- $357
- Updated
- 2024/03/01
- Product number
- V849530
- Product name
- Vadadustat
- Packaging
- 5mg
- Price
- $195
- Updated
- 2021/12/16
Vadadustat Chemical Properties,Usage,Production
Description
Vadadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2) and HIF-PH3 (IC50s = 1.1 and 0.39 micromolar, respectively). It stabilizes HIF-1α in mouse hepatocyte nuclear extracts. Vadadustat (50 and 100 mg/kg) increases erythropoietin levels in mouse serum.
Uses
Vadadustat is a novel HIF (Hypoxia-inducible factor) stabilizer. It provides an effective anemia treatment in nondialysis-dependent chronic kidney disease.
Indications
Vadadustat is used to treat anemia in dialysis-dependent and non-dialysis-dependent chronic kidney disease patients.
Mechanism of action
Vadadustat inhibits PDH and reduces the degradation of HIF-α, thereby increasing the production of endogenous erythropoietin (EPO) and improving anemia symptoms.
Synthesis
Boronic acid 69 and pyridine nitrile 70 were coupled via Suzuki coupling to give biphenyl 71. Crystallization of 71 was required to remove small amounts of undesired regioisomer coupling products. One-pot reaction: aromatic substitution with methoxy anion. Hydrolysis of the nitrile was performed simultaneously. These two independent operations were performed in one pot to give compound 72 in 92% overall yield for the two steps. Carboxylic acid 72 and amine 73 were amidated using CDI (carbodiimide) as coupling agent to give compound 74. Aluminum-mediated demethylation of 74 removed the ester and ether functionalities to give vadadustat (XI) in 84% yield.
Advantages
Vadadustat offers the convenience of traditional injectable EPO stimulators, helping to improve patient compliance with treatment. In clinical trials, Vadadustat has been shown to improve hemoglobin levels in CKD patients and has good safety and tolerability.
References
[1] ROBERT LABES Kameliya R. Prolyl hydroxylase inhibitors, polydrug use, and the phosphoproteome[J]. Acta Physiologica, 2022, 237 1. DOI: 10.1111/apha.13898
Vadadustat Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Vadadustat manufacturers
- Product
- Vadadustat 1000025-07-9
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99.5%
- Supply Ability
- EX：100kg
- Release date
- 2025-07-22
- Product
- Vadadustat 1000025-07-9
- Price
- US $0.00-0.00/g
- Min. Order
- 1g
- Purity
- 98%
- Supply Ability
- 1000kgs
- Release date
- 2021-05-24
- Product
- Vadadustat 1000025-07-9
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-08