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BAY 41-8543
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY 41-8543图片
CAS NO:256498-66-5
规格:98%
分子量:420.4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
heme-dependent stimulator of soluble guanylate cyclase (sGC)
CAS:256498-66-5
分子式:C21H21FN8O
分子量:420.4
纯度:98%
存储:Store at -20°C

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.


参考文献:
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).