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APJ receptor agonist 4

Catalog No. T39587 CAS 2135515-67-0

APJ Receptor Agonist 4 is a potent, orally active apelin receptor (APJ) agonist, demonstrating an EC50 of 0.06 nM and a Ki of 0.07 nM. It exhibits excellent pharmacokinetic profiles in rodent heart failure (HF) models and has shown an acceptable safety profile in preclinical toxicology studies. This compound effectively improves cardiac function, making it valuable for research into HF disease.

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APJ receptor agonist 4 Chemical Structure

APJ receptor agonist 4, CAS 2135515-67-0

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In vivo

This study evaluates the pharmacokinetics (PK) profile of APJ receptor agonist 4 (compound 21) across different species, including mice, rats, monkeys, and dogs. For each species, the research illustrates the maximum plasma concentration (Cmax), dose administered (both intravenously [i.v.] and orally [p.o.]), clearance (CI), steady-state volume of distribution (Vss), half-life (T1/2), the peak concentration time (Cmax) in µM?h, and area under the curve (AUC) from 0 to 24 hours in µM?h. The dosing varied, with 1 mg/kg for both routes in mice, 1 mg/kg (i.v.) and 3 mg/kg (p.o.) in rats, and identical dosing for monkeys and dogs. Two vehicles were used for compound administration: Vehicle F (5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9) and Vehicle G (10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9), affecting the bioavailability (F%) across species—54% in mice, 27% in rats, and 76% in dogs. The study provides a comparative analysis of how compound 21's absorption, distribution, metabolism, and excretion characteristics vary among different animal models.

Molecular Weight	551.02
Formula	C28H28ClFN6O3
CAS No.	2135515-67-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Meng W, et al. Identification of a Hydroxypyrimidinone Compound (21) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure. J Med Chem. 2021;64(24):18102-18113.

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APJ receptor agonist 4 2135515-67-0 inhibitor inhibit

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