产品
编 号：F750887
分子式：C31H26ClN3O3
分子量：524.01
分子式：C31H26ClN3O3
分子量：524.01
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CAS No: 2287153-38-0
产品详情
生物活性：
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
体内研究：
APJ receptor agonist 1 (10-100 μg/min/kg; intravenous infusion) induces a 10% increase in CO with minimal impact on blood pressure (<5% transient blood pressure drop).Animal Model:Isoflurane-anesthetized male Sprague Dawley rats
Dosage:10, 100, 1000 μg/kg/min
Administration:IV; infused into the jugular vein for 15 min
Result:Showed a dose-dependent improvement in the cardiac output in male Sprague Dawley rats with no significant changes in either mean arterial blood pressure or heart rate.
体外研究：
The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer..
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
体内研究：
APJ receptor agonist 1 (10-100 μg/min/kg; intravenous infusion) induces a 10% increase in CO with minimal impact on blood pressure (<5% transient blood pressure drop).Animal Model:Isoflurane-anesthetized male Sprague Dawley rats
Dosage:10, 100, 1000 μg/kg/min
Administration:IV; infused into the jugular vein for 15 min
Result:Showed a dose-dependent improvement in the cardiac output in male Sprague Dawley rats with no significant changes in either mean arterial blood pressure or heart rate.
体外研究：
The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer..
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