Molidustat(BAY 85-3934) Struktur

Molidustat(BAY 85-3934)

Bezeichnung:Molidustat(BAY 85-3934)

CAS-Nr1154028-82-6

Englisch Name:Molidustat(BAY 85-3934)

CBNumberCB72729607

SummenformelC13H14N8O2

Molgewicht314.3

MOL-Datei1154028-82-6.mol

Molidustat(BAY 85-3934) physikalisch-chemischer Eigenschaften

Siedepunkt	589.2±60.0 °C(Predicted)
Dichte	1.67±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in EtOH; insoluble in H2O; ≥5.68 mg/mL in DMF
Aggregatzustand	solid
pka	5.38±0.37(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

Molidustat(BAY 85-3934) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Hypoxia-inducible factor (HIF) is the major transcription factor involved in erythropoietin gene expression. Because oxygen-dependent degradation of the α subunit of HIF suppresses erythropoietin expression, stimulation of erythropoiesis by agents that prevent degradation of HIF has been one strategy for managing anemia. BAY 85-3934 stabilizes HIF from degradation in the proteasome by inhibiting HIF-1α prolyl hydroxylase (IC₅₀ = 0.49 μM). Inhibition of HIF prolyl hydroxylase by BAY 85-3934 has been shown to increase endogenous production of erythropoietin. This compound has been investigated in clinical trial for treatment of patients with anemia associated with chronic kidney disease and/or end-stage renal disease.
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].
IC 50
480 nm, 280 nm, and 450 nm for phd1, phd2, and phd3, respectively.
Einzelnachweise
[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.

Molidustat(BAY 85-3934) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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