1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase

Molidustat (Synonyms: BAY 85-3934)

Cat. No.: HY-12654 Purity: 98.27%
Data Sheet SDS Handling Instructions

Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.

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Molidustat Chemical Structure

Molidustat Chemical Structure

CAS No. : 1154028-82-6

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Description

Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.

IC50 & Target

IC50: 480 nM (PHD1), 280 nM (PHD2), 450 nM (PHD3)[1]

In Vitro

The mean IC50 values of BAY 85-3934 for PHD1, PHD2, and PHD3 are 480 nM, 280 nM, and 450 nM, respectively. Exposure of HeLa cells to 5 μM BAY 85-3934 for 20 min is sufficient to induce detectable concentrations of HIF-1α. In a cellular reporter assay, BAY 85-3934 induces the expression of the firefly luciferase reporter gene under the control of a hypoxia responsive element promoter at a mean (± SD) EC50 of 8.4±0.7 μM (n=4) [1].

In Vivo

HIF stabilization by oral administration of the HIF-PH inhibitor BAY 85-3934 (molidustat) results in dose-dependent production of EPO in healthy Wistar rats and cynomolgus monkeys. Molidustat therapy is aldo 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
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.1817 mL 15.9084 mL 31.8167 mL
5 mM 0.6363 mL 3.1817 mL 6.3633 mL
10 mM 0.3182 mL 1.5908 mL 3.1817 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Rat: BAY 85-3934 is prepared as a solution in ethanol:Solutol HS 15:water (10∶20∶70). In a repeat-dose, 26-day experiment, male Wistar rats (240–340 g in body weight) are administered vehicle or BAY 85-3934 at doses of 0.5 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5 mg/kg. The efficacy of BAY 85-3934 (2.5 mg/kg, once-daily, oral) is also compared with that of rhEPO (25 IU/kg, 50 IU/kg, and 100 IU/kg, twice-weekly, s.c. injection). The time-course of induction of EPO mRNA expression and plasma EPO is determined at baseline and 0.5 h, 1 h, 2 h, 4 h, 6 h, and 8 h after oral administration of a single dose of BAY 85-3934 (5 mg/kg)[1].

Monkey: BAY 85-3934 is prepared as a solution in 0.5% tylose. Male and female cynomolgus monkeys (2.8–5.6 kg in body weight) are administered at doses of 0.5 mg/kg and 1.5 mg/kg at 0 h, 24 h, 48 h, 72 h, and 96 h. Blood samples are taken at 7 h, 31 h, 55 h, 79 h, 103 h, and 168 h. Erythropoietic parameters are also evaluated after a 2-week treatment period with s.c. administration of rhEPO (100 IU/kg twice weekly at days 1, 4, 8, and 11) and BAY 85-3934 (1.5 mg/kg) once daily[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

314.3

Formula

C₁₃H₁₄N₈O₂

CAS No.

1154028-82-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: < 3.3 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Molidustat
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