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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-HIF/HIF Prolyl-hydroxylase-Molidustat
Molidustat

Chemical Structure : Molidustat

CAS No.: 1154028-82-6

Molidustat (BAY 85-3934, BAY 853934)

货号: PC-43140Not For Human Use, Lab Use Only.

Molidustat (BAY 85-3934) is an orally active small molecule inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PHD) with IC50 of 480 nM, 280 nM and 450 nM for PHD1, PHD2, and PHD3, respectively.

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10 mg ¥880 In stock
50 mg ¥1980 In stock
100 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Molidustat (BAY 85-3934) is an orally active small molecule inhibitor of hypoxia inducible factor prolyl hydroxylase (HIF-PHD) with IC50 of 480 nM, 280 nM and 450 nM for PHD1, PHD2, and PHD3, respectively.
Molidustat (BAY 85-3934) causes dose-dependent production of erythropoietin (EPO) in healthy Wistar rats and cynomolgus monkeys, increases hemoglobin levels and shows effectivity in the treatment of renal anemia in rats with impaired kidney function, resultsin normalization of hypertensive blood pressure in rat model of CKD.

物理化学性质&存储条件

分子量 314.3027
分子式 C13H14N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: < 3.3 mg/mL

Chemical Name/SMILES

3H-Pyrazol-3-one, 1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)-

参考文献

1. Flamme I, et al. PLoS One. 2014 Nov 13;9(11):e111838.

2. Beck H, et al. ChemMedChem. 2018 Feb 27. doi: 10.1002/cmdc.201700783.

3. Böttcher M, et al. Br J Clin Pharmacol. 2018 Mar 25. doi: 10.1111/bcp.13584.

4. Gupta N, et al. Am J Kidney Dis. 2017 Jun;69(6):815-826.

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