CGP 20712 dihydrochloride is a potent and selective antagonist of β1-adrenoceptor with IC50 value of 0.7 nM.

≥96%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

solid

β1-AR: IC50 = 0.7 nM; Plasmodium falciparum 3D7: IC50 = 2.51 µM; Plasmodium falciparum D10 : IC50 = 3.16 µM

Soluble in water (50 mM).

β1-adrenoceptor

β1-adrenoceptor is a G-protein coupled receptor and mediates uncoupling protein-1 (UCP1) gene expression induced by norepinephrine (NE).

CGP 20712 dihydrochloride is a potent and selective β1-adrenoceptor antagonist. In neocortical membranes, CGP 20712 A exhibited affinity for β1-adrenoceptor and β2-adrenoceptor with IC50 values of 0.7 and 6700 nM, respectively. In brown adipocytes, CGP-20712A significantly inhibited UCP1 gene expression induced by NE. However, CGP-20712A had no effect on lipolysis. These results suggested that β1-adrenoceptor mediated UCP1 gene expression. In ventricular membranes from rats, CGP 20712A (300 nM) completely occupied its high-affinity binding sites. In ventricular myocytes isolated from rats, CGP 20712A (10, 100, 1000 nM) didn’t cause the activation of adenylate cyclase mediated by β2-adrenoceptors, which suggested that β2-adrenoceptors were not present on rat ventricular myocytes . In adult rat cardiac myocytes, CGP 20712A inhibited β1-AR-stimulated apoptosis, which was mediated by a cAMP-dependent mechanism.