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Molidustat(BAY85-3934)
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。
Molidustat(BAY85-3934)图片
CAS NO:1154028-82-6
规格:98%
分子量:314.3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Novel HIF-PH inhibitor
CAS:1154028-82-6
分子式:C13H14N8O2
分子量:314.3
纯度:98%
存储:Store at -20°C

Background:

Molidustat (BAY85-3934)


Description:


IC50: 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively.


Oxygen sensing via hypoxia-inducible factor prolyl hydroxylases (HIF-PHs) is the dominant regulatory mechanism of erythropoietin (EPO) expression. In chronic kidney disease (CKD), impaired EPO expression causes anemia, which can be treated by supplementation with recombinant human EPO (rhEPO). Molidustat (BAY85-3934) is a novel HIF-PH inhibitor.


In vitro: The IC50 values were found to be dependent on the 2-oxoglutarate concentration in the reaction buffer. By lowering the 2-oxoglutarate concentration from 20 μM to 0.3 μM, the potency of the test compound increased up to 10-fold. Variation of the concentrations of Fe2+ and ascorbate in the reaction buffer by factors of 30 and 200, respectively, did not alter the potency of the inhibitor by more than 2-fold [1].


In vivo: In repeat dosing of BAY 85-3934, hemoglobin levels were increased compared with animals in vehicle group, while endogenous EPO remained within the normal physiological range. BAY 85-3934 therapy was also effective in the treatment of renal anemia in rats with impaired kidney function and, unlike treatment with rhEPO, resulted in normalization of hypertensive blood pressure in a rat model of CKD [1].


Clinical trial: Clinical studies are still ongoing to investigate the effects of BAY 85-3934 therapy in patients with renal anemia (https://clinicaltrials.gov/ct2/show/NCT01332942?term=Molidustat&rank=2).


Reference:
[1] Flamme I, Oehme F, Ellinghaus P, Jeske M, Keldenich J, Thuss U.  Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects. PLoS One. 2014 Nov 13;9(11):e111838.