Company Name: |
Shanghai Kewel Chemical Co., Ltd.
|
Tel: |
021-64609169 18901607656 |
Email: |
greensnown@163.com |
Products Intro: |
Product Name:Roxadustat-d5 CAS:2043026-13-5 Purity:95+ HPLC; Package:10mg;25mg;50mg;100mg
|
Company Name: |
QUALITY CONTROL SOLUTIONS LTD.
|
Tel: |
13670046396 |
Email: |
ORDERS@QCSRM.COM |
Products Intro: |
Product Name:Roxadustat-d5 CAS:2043026-13-5 Purity:95% HPLC Package:10MG;25MG;50MG;100MG
|
Company Name: |
ChemeGen 中国
|
Tel: |
18818260767 |
Email: |
sales@chemegen.com |
Products Intro: |
Product Name:Roxadustat-d5 CAS:2043026-13-5 Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
|
Company Name: |
Beijing Biocreative Technology Co., Ltd.
|
Tel: |
15522676233 |
Email: |
3007606172@qq.com |
Products Intro: |
Product Name:Roxadustat-d5 CAS:2043026-13-5 Purity:99% HPLC Package:1.0mg; 10.0mg; 25.0mg; 50.0mg; 100.0mg; 200.0mg; 500.0mg; 2.0g; 5.0g;
|
|
| Roxadustat-d5 Basic information |
| Roxadustat-d5 Chemical Properties |
storage temp. | -20°C | solubility | Acetone: soluble,DMSO: soluble | form | A solid | color | White to off-white |
| Roxadustat-d5 Usage And Synthesis |
Uses | Roxadustat-D5 is a useful research chemical compound used in the preparation of deuterium containing isoquinolinecarboxamide derivatives useful for the treatment of anemia and hemocyte related diseases. | Biological Activity | Roxadustat-d5 is 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).1 It 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.2 Roxadustat 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 | References | 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) |
| Roxadustat-d5 Preparation Products And Raw materials |
|