| BAY 41-8543heme-dependent stimulator of soluble guanylate cyclase (sGC) |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 256498-66-5 | SDF | Download SDF |
| Chemical Name | 2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-(4-morpholinyl)-4,6-pyrimidinediamine | ||
| Canonical SMILES | FC(C=CC=C1)=C1CN2N=C(C3=NC(N)=C(N4CCOCC4)C(N)=N3)C5=C2N=CC=C5 | ||
| Formula | C21H21FN8O | M.Wt | 420.4 |
| Solubility | ≤3mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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).
