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CAS No.: 1262132-81-9

Enarodustat Catalog No. CSN22394

Synonyms: JTZ-951

Enarodustat is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia.

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技术信息

生物活性

描述The hypoxia signalling pathway enables adaptation of cells to decreased oxygen availability. When oxygen becomes limiting, the central transcription factors of the pathway, hypoxia-inducible factors (HIFs), are stabilised and activated to induce the expression of hypoxia-regulated genes, thereby maintaining cellular homeostasis^[1].Enarodustat (JTZ-951) is an oral hypoxia-inducible factor prolyl hydroxylase inhibitor that mimics adaptive responses to hypoxic conditions and may provide a new therapeutic approach for managing anemia in patients with chronic kidney disease (CKD)^[2].Fatty acid and amino acid metabolisms were upregulated in diabetic renal tissue and downregulated by enarodustat, whereas glucose metabolism was upregulated.Whereas glycolysis and tricarboxylic acid cycle metabolites were accumulated and amino acids reduced in renal tissue of diabetic animals, these metabolic disturbances were mitigated by enarodustat. Furthermore, enarodustat increased the glutathione to glutathione disulfide ratio and relieved oxidative stress in renal tissue of diabetic animals^[3].Compared with brachyury ob/ob mice that received only vehicle, BTBR ob/ob mice treated with enarodustat displayed lower body weight, reduced blood glucose levels with improved insulin sensitivity, lower total cholesterol levels, higher adiponectin levels, and less adipose tissue, as well as a tendency for lower macrophage infiltration. Enarodustat-treated mice also exhibited reduced albuminuria and amelioration of glomerular epithelial and endothelial damage^[4].
参考文献

[1] Adam Albanese,et al. The Role of Hypoxia-Inducible Factor Post-Translational Modifications in Regulating Its Localisation, Stability, and Activity. Int J Mol Sci. 2020 Dec 29;22(1):268.
[2] Tadao Akizawa,et al. A Placebo-Controlled, Randomized Trial of Enarodustat in Patients with Chronic Kidney Disease Followed by Long-Term Trial. Am J Nephrol. 2019;49(2):165-174.
[3] Sho Hasegawa,et al. The oral hypoxia-inducible factor prolyl hydroxylase inhibitor enarodustat counteracts alterations in renal energy metabolism in the early stages of diabetic kidney disease Kidney Int. 2020 May;97(5):934-950.
[4] Mai Sugahara,et al. Prolyl Hydroxylase Domain Inhibitor Protects against Metabolic Disorders and Associated Kidney Disease in Obese Type 2 Diabetic Mice. J Am Soc Nephrol. 2020 Mar;31(3):560-577.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9383 mL
- 14.6915 mL
- 29.3830 mL
- 5 mM
- 0.5877 mL
- 2.9383 mL
- 5.8766 mL
- 10 mM
- 0.2938 mL
- 1.4691 mL
- 2.9383 mL

技术信息

CAS号

1262132-81-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16N4O4

运输

蓝冰

分子量

340.33

别名

JTZ-951

溶解度

DMSO	68.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (5.9 mM)

动物实验配方

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