Molidustat sodium

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Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC₅₀ values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia.

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Molidustat sodium Chemical Structure

CAS No. : 1375799-59-9

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Molidustat

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6 Publications Citing Use of MCE Molidustat sodium

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HIF-1α HIF

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Description	Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC₅₀ values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia^[1]^[2].
IC₅₀ & Target	IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)^[1]
In Vitro	Molidustat sodium (5 μM; 20 min) is sufficient to induce detectable levels of HIF-1α in HeLa cells. In a cell reporter assay, Molidustat sodium induces expression of a firefly luciferase reporter gene under the control of a hypoxia response element promoter with a mean (± SD) EC50 of 8.4 μM (n=4)^[1] MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Molidustat sodium Related Antibodies
In Vivo	Molidustat sodium, by stabilizing the hypoxia-inducible factor (HIF), leads to a dose-dependent increase in erythropoietin (EPO) in both Wistar rats (0.5-5 mg/kg; oral; once daily for 26 days) and cynomolgus monkeys (0.5-1.5mg/kg; once daily for 5 days)^[1]. Molidustat sodium (0.5-10 mg/kg; orally; five times weekly) can normalize the blood pressure in rat models of chronic kidney disease (CKD) and effectively alleviate renal anemia in rats with impaired renal function^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	336.28
Formula	C₁₃H₁₃N₈NaO₂
CAS No.	1375799-59-9
SMILES	[Na]OC1=C(N2N=NC=C2)C=NN1C3=NC=NC(N4CCOCC4)=C3
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (273 KB) Handling Instructions (2659 KB)
References	[1]. Flamme I, et al. 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. [Content Brief] [2]. Yamamoto H,et al. Molidustat for Renal Anemia in Nondialysis Patients Previously Treated with Erythropoiesis-Stimulating Agents: A Randomized, Open-Label, Phase 3 Study. Am J Nephrol. 2021;52(10-11):884-893. [Content Brief]