Molidustat


Catalog No. size PriceQuantity
M6679-2 2mg solid $93
M6679-10 10mg solid $356

Description

Cas:1154028-82-6

Product Information

Molidustat, also known as BAY 85-3934, is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. Phase I data have shown that inhibition of HIF-PH by Molidustat results in an increase in endogenous production of EPO. Molidustat is currently clinical trials at Bayer for the treatment of patients suffering from renal anemia due to chronic kidney disease.

 

Chemical Formula: C13H14N8O2

 

Exact Mass: 314.12397

 

Molecular Weight: 314.3

 

Elemental Analysis: C, 49.68; H, 4.49; N, 35.65; O, 10.18

 

Synonym: 

 

BAY 85-3934;

BAY-85-3934;

BAY85-3934;

BAY 853934;

BAY-853934;

BAY853934;

Molidustat.

 

Chemical Name:

2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one

 

InChi Key:

IJMBOKOTALXLKS-UHFFFAOYSA-N

 

InChi Code:

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

 

Smiles Code:

O=C1N(C2=NC=NC(N3CCOCC3)=C2)NC=C1N4N=NC=C4

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, DMF, and 1:1 DMF:PBS

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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).

 

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.

 

 

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.

 

Products are for research use only. Not for human use.

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