2. GPCR/G Protein
  3. Apelin Receptor (APJ)

Apelin Receptor (APJ)

Apelin receptor (APJ) is a member of the family A of G-protein-coupled receptors (GPCRs) and Apelin is an endogenous ligand for an APJ that was previously isolated from bovine stomachs. Apelin is a 77-amino acid precursor protein that is hydrolysed to produce active peptides of different lengths, such as Apelin-36, Apelin-31, Apelin-17, and Apelin13. The apelin/APJ system plays important roles in the physiology and pathophysiology of several organs, including regulation of fluid homeostasis, blood pressure, cardiac contractility, angiogenesis, metabolic balance, and cell proliferation, apoptosis, or inflammation. Additionally, the apelin/APJ system is widely expressed in the central nervous system, especially in neurons and oligodendrocytes. APJ is also involved in anxiety, and depression.

Apelin Receptor (APJ) Related Products (48):

Cat. No. Product Name Effect Purity
  • HY-109111
    Azelaprag Agonist 99.94%
    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[1].
  • HY-139485
    BMS-986224 99.33%
    BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr1) apelin-13. BMS-986224 has the potential for the research of heart failure[1].
  • HY-P1033
    [Pyr1]-Apelin-13 Agonist 99.92%
    [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.
  • HY-P1944A
    Apelin-13 TFA Agonist 99.53%
    Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC 50 value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome[1][2][3].
  • HY-103254
    ML221 Antagonist
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-P5392A
    Apelin-16, human, bovine acetate
    Apelin-16, human, bovine acetate is a biological active peptide. (Apelin is the endogenous ligand for the G-protein-coupled APJ receptor. It is produced as a pre-proprotein of 77 amino acids.Apelin-16 is one of the active fragment of Apelin).
  • HY-170419
    APJ receptor agonist 10 Agonist
    APJ receptor agonist 10 (Compound I choline salt) modulates the activity of APJ receptor and can be used in research about pulmonary arterial hypertension. APJ receptor agonist 10 exhibits good bioavailability other than its free base form[1].
  • HY-169752
    APJ receptor agonist 11 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[1].
  • HY-139876
    APJ receptor agonist 3 Agonist
    APJ receptor agonist 3 is a potent and orally active APJ receptor agonist with an EC50 value of 0.027 nM.
  • HY-122197
    ML339 Antagonist 99.88%
    ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research[1][2].
  • HY-126293
    Apelin agonist 1 Agonist
    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[1].
  • HY-P3346
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) Agonist
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki 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[1].
  • HY-P2196
    ELA-32(human) Chemical
    ELA-32 (human) is a potent critical cardiac developmental peptide that acts through the G-protein–coupled apelin receptor[1].
  • HY-103080
    CMF019 Agonist 99.89%
    CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi 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[1]. 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[1][2][3][4].
  • HY-P2271
    MM 54 Inhibitor 99.16%
    MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation[1][2].
  • HY-147751
    APJ receptor agonist 6 Agonist
    APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki 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[1].
  • HY-P7061A
    ALX 40-4C Trifluoroacetate Inhibitor
    ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.
  • HY-P2249
    ELA-21 (human) Agonist 98.92%
    ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways[1].
  • HY-160076
    APJ receptor agonist 8 Agonist
    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[1].
  • HY-P3162
    (Ala13)-Apelin-13 Antagonist
    (Ala13)-Apelin-13 is a potent apelin receptors (APJ) antagonist. (Ala13)-Apelin-13 inhibits gastric motility through vagal cholinergic pathway[1].