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256498-66-5

256498-66-5 Structure

256498-66-5 Structure
IdentificationBack Directory
[Name]

BAY-41-8543
[CAS]

256498-66-5
[Synonyms]

BAY-41-8543
BAY-41-8543 Exclusive
BAY 41-8543 (BAY 418543)
2-[1-[(2-fluorophenyl)methyl]pyrazolo[3,4-b]pyridin-3-yl]-5-morpholin-4-ylpyrimidine-4,6-diamine
2-[1-[(2-Fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-4,6-pyrimidinediamine
4,6-Pyrimidinediamine, 2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-
BAY 418543,vascular,systemic,antiplatelet,vasodilator,soluble,pulmonary,orally,nitric,beds,cardiovascular,BAY 41 8543,Guanylate Cyclase,Inhibitor,sGC,BAY 41-8543,oxide,inhibit
[Molecular Formula]

C21H21FN8O
[MDL Number]

MFCD18382081
[MOL File]

256498-66-5.mol
[Molecular Weight]

420.44
Chemical PropertiesBack Directory
[Boiling point ]

599.7±50.0 °C(Predicted)
[density ]

1.55±0.1 g/cm3(Predicted)
[solubility ]

DMF: 3 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml
[form ]

A crystalline solid
[pka]

5.18±0.10(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Uses]

BAY 41-8543, is a Guanylyl cyclase (sGC) stimulator, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold. BAY 41-8543 reduces pulmonary vascular resistance and protects right ventricular (RV)function. It also inhibits collagen-induced platelet aggregation, and promotes lipid uptake into brown adipose tissue and increases energy expenditure in mice. It has also shown Antihypertensive activity.
[Definition]

ChEBI: BAY-41-8543 is a pyrazolopyridine.
[in vivo]

BAY 41-8543 (10-100 μg/kg; IV) produces small decreases in pulmonary arterial pressure, larger dose-dependent decreases in systemic arterial pressure, and increases in cardiac output[1].
BAY 41-8543 (0.003, 0.01, 0.03, 0.1, and 0.3?mg/kg; iv) produces a dose-dependent and long-lasting decrease in blood pressure in anaesthetized rats. The blood pressure lowering effect of BAY 41-8543 lasts longer than the observation period of 30?min. BAY 41-8543 (0.1, 0.3 and 1.0?mg?kg; oral) has maximal blood pressure lowering effects. The blood pressure lowering effects of the highest doses of BAY41-8543 lasts longer than the observation period of 120?min[2].
BAY 41-8543 (3?mg/kg; p.o.; twice daily; for 5 weeks) completely prevents the development of the increase in systolic blood pressure in 18-week-old renin transgenic rats (TGR(mRen2)27) on L-NAME treatment. BAY 41-8543 dramatically increases survival[2].

Animal Model:Adult male Sprague-Dawley rats weighing 325-450 g[1]
Dosage:10, 30, and 100 μg/kg
Administration:IV
Result:Produced small decreases in pulmonary arterial pressure, larger dose-dependent decreases in systemic arterial pressure, and increases in cardiac output.
[storage]

Store at -20°C
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