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APJ receptor agonist 1

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Catalog No. T39813Cas No. 2287153-38-0

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.

APJ receptor agonist 1

APJ receptor agonist 1

😃Good
Catalog No. T39813Cas No. 2287153-38-0
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.
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Product Introduction

Bioactivity
Description
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.
In vitro
The S-atropisomer of APJ receptor agonist 1 (compound 15a) exhibits 200 times greater potency than its R-atropisomer counterpart.[1].
In vivo
APJ receptor agonist 1, administered via intravenous infusion at dosages of 10-100 μg/min/kg, resulted in a 10% enhancement of cardiac output (CO) with negligible effects on blood pressure, specifically less than a 5% transient reduction. This outcome was observed in isoflurane-anesthetized male Sprague Dawley rats. The administration involved infusing the compound into the jugular vein for 15 minutes, demonstrating a dose-dependent increase in cardiac output without significant alterations in mean arterial blood pressure or heart rate[1].
Chemical Properties
Molecular Weight524.02
FormulaC31H26ClN3O3
Cas No.2287153-38-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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