Apelin Receptor (APJ) Agonist

APJ receptor agonist 3 is a potent and orally active APJ receptor agonist with an EC₅₀ value of 0.027 nM.

APJ receptor agonist 10 free base is an agonist of the APJ Receptor. APJ receptor agonist 10 free base can be used for research on pulmonary arterial hypertension.

Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0.

NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a K_i of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) can activate Gαi1 (EC₅₀=0.8 nM) and recruit β-arrestin2 (EC₅₀=31 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) exhibits prolonged cardiac effects.

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i of 1.3 μM. APJ receptor agonist 6 has EC₅₀ values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.

APJ receptor agonist 8 (compound 99) is an agonist of APJ receptor. APJ receptor agonist 8 increases the load independent cardiac contractility of isolated perfused rat hearts.

Apelin agonist 2 (Compound 35) is an orally active APLNR agonist. Apelin agonist 2 can significantly inhibit the accumulation of cAMP (EC₅₀ = 10 nM). Apelin agonist 2 exhibits a significant improvement in glucose tolerance. Apelin agonist 2 can be used to study metabolic diseases such as diabetes.

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.

Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC₅₀ of 5.4 nM, and potently inhibits cAMP production with an EC₅₀ of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.

Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC₅₀=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.

AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (K_i=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life.

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.

Azelaprag (Standard) is the analytical standard of Azelaprag (HY-109111). This product is intended for research and analytical applications. Azelaprag (Example 263.0) is a candidate active molecule for an Apelin receptor agonist with an EC₅₀ of 0.32 nM for the apelin receptor.

Pyr1]-Apelin-13, Gly(15N) TFA is a Gly¹⁵N labeled [Pyr1]-Apelin-13. [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor agonist.

APJ receptor agonist 11 (Ex 174) is a APJ receptor agonist with IC₅₀ values ranging from 0.01 nM to 10 nM. APJ receptor agonist 11 can be used in the study of cardiovascular diseases.

CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pK_i values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension.