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Vadadustat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Vadadustat图片
CAS NO:1000025-07-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Vadadustat (PG-1016548) 是一种可滴定的口服缺氧诱导因子脯氨酰羟化酶 (HIF-PH) 抑制剂。
Cas No.1000025-07-9
别名伐度司他,PG-1016548; AKB-6548
化学名2-(5-(3-chlorophenyl)-3-hydroxypicolinamido)acetic acid
Canonical SMILESOC1=CC(C2=CC=CC(Cl)=C2)=CN=C1C(NCC(O)=O)=O
分子式C14H11ClN2O4
分子量306.7
溶解度DMF: 5mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04mg/mL,DMSO: 2mg/mL,Ethanol: 2mg/mL
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

Vadadustat induces endogenous erythropoietin synthesis and enhances iron mobilization. Vadadustat is well-tolerated in healthy volunteers and patients with chronic kidney disease, where it increases reticulocytes, plasma EPO, and Hb levels in a dose-dependent manner. The increase in plasma EPO levels seen with vadadustat is comparable in magnitude to that occurring physiologically at moderate altitude and shows a normal diurnal pattern with a return to baseline levels prior to the next dose. Vadadustat improves iron homeostasis by decreasing hepcidin and increasing transferrin levels. once-daily oral administration of vadadustat, titrated to increase and maintain Hb in the target range, may provide multiple advantages over conventional ESAs[1]. Vadadustat is observed to have a half-life of approximately 4.5 hours. Overall, patients demonstrate an increase in Hb levels, from 9.91 g/dL at baseline to 10.54 g/dL by day 29. Ferritin levels decrease from 334.1 ng/mL at baseline to 271.7 ng/mL by day 29[2].

References:
[1]. Pergola PE, et al. Vadadustat, a novel oral HIF stabilizer, provides effective anemia treatment in nondialysis-dependent chronic kidney disease. Kidney Int. 2016 Nov;90(5):1115-1122.
[2]. Gupta N, et al. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors: A Potential New Treatment for Anemia in Patients With CKD. Am J Kidney Dis. 2017 Feb 24. pii: S0272-6386(17)30110-5.