Merck, 196876-5MG, BAY 41-2272

General description
A cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 µM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α₁ and α₂ subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC₅₀ = 304 nM) and blocks collagen-induced aggregation of human platelets (IC₅₀ = 36 nM). Does not inhibit phosphodiesterases.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Soluble guanylate cyclase
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 304 nM inhibiting phenylephrine-induced constriction of rabbit aortic rings; 36 nM in blocking collagen-induced aggregation of human platelets
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Boerrigter, G., et al. 2003. Circulation107, 686.
Kalsi, J.S., et al. 2003. J Urol.169, 761.
Koglin, M., et al. 2002. Biochem. Biophys. Res. Commun.292, 1057.
Becker, E.M., et al. 2001. BMC Pharmacol.1, 13.
Stasch, J.P., et al. 2001. Nature410, 212.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)