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Molidustat (BAY85-3934)

Novel HIF-PH inhibitor CAS# 1154028-82-6

Molidustat (BAY85-3934)

Catalog No. BCC6412----Order now to get a substantial discount!

Product Name & Size Price Stock
Molidustat (BAY85-3934):5mg $98.00 In stock
Molidustat (BAY85-3934):10mg $167.00 In stock
Molidustat (BAY85-3934):25mg $392.00 In stock
Molidustat (BAY85-3934):50mg $686.00 In stock
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Quality Control of Molidustat (BAY85-3934)

Quality Control & MSDS

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Chemical structure

Molidustat (BAY85-3934)

3D structure

Chemical Properties of Molidustat (BAY85-3934)

Cas No. 1154028-82-6 SDF Download SDF
PubChem ID 59603622 Appearance Powder
Formula C13H14N8O2 M.Wt 314.3
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BAY 85-3934
Solubility DMSO : 5 mg/mL (15.91 mM; Need ultrasonic)
Chemical Name 2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one
SMILES C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4
Standard InChIKey IJMBOKOTALXLKS-UHFFFAOYSA-N
Standard InChI InChI=1S/C13H14N8O2/c22-13-10(20-2-1-16-18-20)8-17-21(13)12-7-11(14-9-15-12)19-3-5-23-6-4-19/h1-2,7-9,17H,3-6H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Molidustat (BAY85-3934)

DescriptionMolidustat (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.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].

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.

Protocol

Animal Administration [1]
Rats: 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].

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.

Molidustat (BAY85-3934) Dilution Calculator

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Preparing Stock Solutions of Molidustat (BAY85-3934)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1817 mL 15.9084 mL 31.8167 mL 63.6335 mL 79.5418 mL
5 mM 0.6363 mL 3.1817 mL 6.3633 mL 12.7267 mL 15.9084 mL
10 mM 0.3182 mL 1.5908 mL 3.1817 mL 6.3633 mL 7.9542 mL
50 mM 0.0636 mL 0.3182 mL 0.6363 mL 1.2727 mL 1.5908 mL
100 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.6363 mL 0.7954 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Molidustat (BAY85-3934)

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.

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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.

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