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APJ receptor agonist 4

APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease[1].

Product Specifications

CAS Number

2762567-70-2

UNSPSC

12352005

Target

Apelin Receptor (APJ)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/apj-receptor-agonist-4.html

Solubility

10 mM in DMSO

Smiles

O=C1C(C(N2CC[C@@H](C3=C(F)C=C(Cl)C=N3)C2)=O)=C(O)N(C4=C(CC)C=CC=C4CC)C(C5=NN(C)C=C5)=N1

Molecular Formula

C28H28ClFN6O3

Molecular Weight

551.01

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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