Powder: -20°C for 3 years | In solvent: -80°C for 1 year
APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research.
产品描述 | APJ receptor agonist 1, a potent biphenyl acid derivative, acts as an agonist (EC50 of 0.093 nM and 0.12 nM for human and rat APJ receptors, respectively) for the APJ receptor (APJ-R). It exhibits significant in vitro potency towards apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 holds promise for heart failure research. |
体外活性 | The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer.[1]. |
体内活性 | 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)[1]. Animal Model: Isoflurane-anesthetized male Sprague Dawley rats[1]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. |
分子量 | 524.02 |
分子式 | C31H26ClN3O3 |
CAS No. | 2287153-38-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
APJ receptor agonist 1 2287153-38-0 Inhibitor inhibitor inhibit