产品
编 号：F271779
分子式：C30H48N2O6
分子量：532.71
分子式：C30H48N2O6
分子量：532.71
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CAS No: 212481-66-8
产品详情
生物活性：
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
体内研究：
ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats.Animal Model:Male Sprague-Dawley rats (250-350 g) induced with endothelin-1
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:Oral administration; for 1 hour or 4 hours
Result:Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
体外研究：
ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETA receptor in membranes prepared from rat pituitary MMQ cells with an IC50 value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBrceptor in membranes prepared from porcine cerebellum with an IC50value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ETAand ETBreceptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETAreceptor with an IC50value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBreceptor with an IC50value of 15,400 nM.In isolated vessels, ABT-546 inhibits endothelin ETA receptor-mediated endothelin-1-induced vasoconstriction, and endothelin ETB receptor-mediated sarafotoxin 6c-induces vasoconstriction with pA2of 8.29 and 4.57, respectively.
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
体内研究：
ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats.Animal Model:Male Sprague-Dawley rats (250-350 g) induced with endothelin-1
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:Oral administration; for 1 hour or 4 hours
Result:Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
体外研究：
ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETA receptor in membranes prepared from rat pituitary MMQ cells with an IC50 value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBrceptor in membranes prepared from porcine cerebellum with an IC50value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ETAand ETBreceptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETAreceptor with an IC50value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBreceptor with an IC50value of 15,400 nM.In isolated vessels, ABT-546 inhibits endothelin ETA receptor-mediated endothelin-1-induced vasoconstriction, and endothelin ETB receptor-mediated sarafotoxin 6c-induces vasoconstriction with pA2of 8.29 and 4.57, respectively.
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