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Roxadustat-d5
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。
Roxadustat-d5图片
CAS NO:2043026-13-5
包装:1mg
市场价:5670元

产品介绍
Roxadustat-d5 是氘标记的 Roxadustat。 Roxadustat 是一种口服缺氧诱导因子脯氨酰羟化酶抑制剂 (HIF-PHI),通过增加内源性红细胞生成素、改善铁调节和减少铁调素来促进红细胞生成。
Cas No.2043026-13-5
Canonical SMILESCC1=NC(C(NCC(O)=O)=O)=C(O)C2=C1C=C(OC3=C([2H])C([2H])=C([2H])C([2H])=C3[2H])C=C2
分子式C19H11D5N2O5
分子量357.4
溶解度Acetone: soluble,DMSO: soluble
储存条件-20°C
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

Roxadustat-d5is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively).1It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg/kg.2Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5/6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcinoma model when administered at a dose of 3 mg/animal.3

1.Yeh, T.-L., Leissing, T.M., Abboud, M.I., et al.Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trialsChem. Sci.8(11)7651-7668(2017) 2.Del Balzo, U., Signore, P.E., Walkinshaw, G., et al.Nonclinical characterization of the hypoxia-inducible factor prolyl hydroxylase inhibitor roxadustat, a novel treatment of anemia of chronic kidney diseaseJ. Pharmacol. Exp. Ther.374(4)342-353(2020) 3.Nishide, S., Matsunaga, S., Shiota, M., et al.Controlling the phenotype of tumor-infiltrating macrophages via the PHD-HIF axis inhibits tumor growth in a mouse modeliScience19940-954(2019)