Desidustat
(Synonyms: ZYAN1) 目录号 : GC32449
An inhibitor of HIF-PH
Cas No.:1616690-16-4
Sample solution is provided at 25 µL, 10mM.
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Desidustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH).1 It reduces levels of hypoxia-inducible factor-1α (HIF-1α), a transcription factor regulated by HIF-PH enzymes, in rat liver and kidney. Desidustat increases the expression of the red blood cell- and iron transport-related genes Epo, Fpn1, and Hamp in rat liver in a model of anemia induced by peptidoglycan-polysaccharide (PGPS).2 It increases plasma levels of erythropoietin in rats by 10.3- to 40-fold when administered at doses of 15 and 30 mg/kg, respectively.1 Desidustat (15 and 30 mg/kg) also increases plasma levels of erythropoietin and hemoglobin, as well as the number of circulating red blood cells, in nephrectomized rats in a model of chronic kidney disease-induced anemia. It increases hemoglobin levels and the number of circulating red blood cells in a mouse model of anemia induced by the DNA-crosslinking agent cisplatin .
1.Jain, M.R., Joharapurkar, A.A., Pandya, V., et al.Pharmacological characterization of ZYAN1, a novel prolyl hydroxylase inhibitor for the treatment of anemiaDrug Res. (Stuttg.)66(2)107-112(2016) 2.Jain, M., Joharapurkar, A., Patel, V., et al.Pharmacological inhibition of prolyl hydroxylase protects against inflammation-induced anemia via efficient erythropoiesis and hepcidin downregulationEur. J. Pharmacol.843113-120(2019)
| Cas No. | 1616690-16-4 | SDF | |
| 别名 | ZYAN1 | ||
| Canonical SMILES | O=C(O)CNC(C1=C(O)C2=C(N(OCC3CC3)C1=O)C=CC=C2)=O | ||
| 分子式 | C16H16N2O6 | 分子量 | 332.31 |
| 溶解度 | DMSO : ≥ 30 mg/mL (90.28 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL |
| 5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL |
| 10 mM | 0.3009 mL | 1.5046 mL | 3.0092 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet