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BAY 41-8543

Catalog No.
C3639
heme-dependent stimulator of soluble guanylate cyclase (sGC)
Grouped product items
SizePriceStock Qty
10mg
$331.00
Ship with 5-10 days
50mg
$1,394.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

IC50: 0.09 μM human platelets

BAY 41-8543 is a soluble guanylate cyclase (sGC) stimulator.

Soluble guanylate cyclase (sGC) has been identified as the primary cellular receptor for nitric oxide (NO). NO can bind and activate a heme group in sGC, initiating the conversion of GTP to the second messenger cyclic GMP (cGMP).

In vitro: Previous study found that BAY 41-8543 could concentration-dependently stimulate the recombinant sGC up to 92-fold. Moreover, BAY 41-8543 and NO had synergistic effects over a wide range of concentrations. Similar results were shown that BAY 41-8543 stimulated the sGC directly and further made the enzyme more sensitive to its endogenous activator NO. In addition, BAY 41-8543 was found to be a potent relaxing agent of aortas, saphenous arteries, coronary arteries and veins with IC50-values in the nm range [1].

In vivo: In anaesthetized dogs, i.v. injections of BAY 41-8543 could cause a dose-dependent decrease in blood pressure and cardiac oxygen consumption as well as an increase in coronary blood flow and heart rate. In anaesthetized normotensive rats, BAY 41-8543 produced a dose-dependent and long-lasting blood pressure lowering effect. Moreover, a dose-dependent and long-lasting decrease in blood pressure was also observed in conscious spontaneously hypertensive rats with a threshold dose of 0.1 mg/kg p.o. [2].

Clinical trial: So far, no clinical study has been conducted.

References:
1.  Stasch, J.P.,Alonso-Alija, C.,Apeler, H., et al. Pharmacological actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: In vitro studies. British Journal of Pharmacology 135, 333-343 (2002).
2.  Stasch, J.P.,Dembowsky, K.,Perzborn, E., et al. Cardiovascular actions of a novel NO-independent guanylyl cyclase stimulator, BAY 41-8543: in vivo studies. British Journal of Pharmacology 135, 344-355 (2002).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt420.4
Cas No.256498-66-5
FormulaC21H21FN8O
Solubility≤3mg/ml in dimethyl formamide
Chemical Name2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-4,6-pyrimidinediamine
SDFDownload SDF
Canonical SMILESFC(C=CC=C1)=C1CN2N=C(C3=NC(N)=C(N4CCOCC4)C(N)=N3)C5=C2N=CC=C5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Quality Control

Quality Control & MSDS

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Chemical structure

BAY 41-8543