バダデュスタット
バダデュスタット 物理性質
- 融点 :
- 172-174°C
- 沸点 :
- 674.6±55.0 °C(Predicted)
- 比重(密度) :
- 1.461±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 酸解離定数(Pka):
- 4.09±0.40(Predicted)
- 外見 :
- 個体
- 色:
- ペールベージュからライトベージュ
- 安定性：:
- 吸湿性
- 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
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
バダデュスタット 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
バダデュスタット 化学特性,用途語,生産方法
効能
貧血治療薬, プロリン水酸化酵素阻害薬
説明
Vadadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2) and HIF-PH3 (IC
50s = 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.
使用
Vadadustat is a novel HIF (Hypoxia-inducible factor) stabilizer. It provides an effective anemia treatment in nondialysis-dependent chronic kidney disease.
作用機序
Vadadustat inhibits PDH and reduces the degradation of HIF-α, thereby increasing the production of endogenous erythropoietin (EPO) and improving anemia symptoms.
安全性
Phase 3 clinical trials in Japan have confirmed the efficacy and safety of vadadustat for the treatment of renal anemia in patients with both non-dialysis-dependent (NDD)-chronic kidney disease (CKD) and dialysis-dependent CKD. The incidence of adverse events (AEs) and serious AEs in the vadadustat treatment group was comparable to that observed in the erythropoiesis-stimulating agents (ESA) treatment group
[2].
合成
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.
バダデュスタット 上流と下流の製品情報
原材料
準備製品
バダデュスタット 生産企業
Global( 114)Suppliers
1000025-07-9(バダデュスタット)キーワード:
- 1000025-07-9
- AKB-6548; AKB 6548; AKB6548; PG-1016548; PG 1016548; PG1016548; B-506; B506; VADADUSTAT
- PG-1016548;AKB-6548
- Vadadustat
- Vadadustat(AKB-6548/PG-1016548)
- Vadadustat (AKB-6548)
- AKB-6548
- PG 1016548
- PG1016548
- PG-1016548
- PG-1016548; PG1016548; PG 1016548; AKB-6548
- CS-2486
- Glycine, N-[[5-(3-chlorophenyl)-3-hydroxy-2-pyridinyl]carbonyl]-
- Vadadustat USP/EP/BP
- Vadadustat (PG-1016548
- Vadadustat 13C6
- Valdesta
- disease,HIFs,AKB 6548,Erythropoiesis-stimulating,kidney,Inhibitor,AKB6548,inhibit,Vadadustat,HIF-PH,PG 1016548,anemia,Hypoxia-inducible factors,PG1016548,nondialysis-dependent,HIF/HIF Prolyl-Hydroxylase,chronic
- Vardorestat
- 2-[[[5-(3-Chlorophenyl)-3-hydroxypyridin-2-yl]carbonyl]amino]acetic acid
- (5-(3-chlorophenyl)-3-hydroxypicolinoyl)glycine
- 2-(5-(3-chlorophenyl)-3-hydroxypicolinamido)acetic acid
- N-[[5-(3-Chlorophenyl)-3-hydroxy-2-pyridinyl]carbonyl]glycine (ACI)
- バダデュスタット
- バダデュスタット (JAN)
- 2-{[5-(3-クロロフェニル)-3-ヒドロキシピリジン-2-イル]ホルムアミド}酢酸
- [[3-ヒドロキシ-5-(3-クロロフェニル)-2-ピリジルカルボニル]アミノ]酢酸