2. Signaling Pathways
  3. GPCR/G Protein
  4. 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 (41):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    Apelin-13 TFA
  • HY-109111
    Azelaprag
    		Agonist 99.84%
    Azelaprag (Example 263.0) is an apelin receptor agonist agent candidate.
    Azelaprag
  • HY-103254
    ML221
    		Antagonist 99.55%
    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.
    ML221
  • HY-P1033
    [Pyr1]-Apelin-13
    		Agonist 99.92%
    [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.
    [Pyr1]-Apelin-13
  • HY-139485
    BMS-986224
    		98.82%
    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.
    BMS-986224
  • HY-P1033S
    [Pyr1]-Apelin-13, Gly(15N) TFA
    		Agonist
    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.
    [Pyr1]-Apelin-13, Gly(15N) TFA
  • HY-W745504
    2-Phenylphenol-d5
    		Agonist
    2-Phenylphenol-d5 is the deuterium labeled 2-Phenylphenol.
    2-Phenylphenol-d<sub>5</sub>
  • 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.
    ML339
  • HY-103080
    CMF019
    		Agonist 98.90%
    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. 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.
    CMF019
  • HY-108003
    MM 07
    		Agonist 99.84%
    MM 07 is a biased apelin receptor agonist, with a KD of 300 nM in CHO-K1 cells and a KD of 172 nM in human heart.
    MM 07
  • HY-P2196A
    ELA-32(human) TFA
    		Agonist 99.27%
    ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
    ELA-32(human) TFA
  • HY-P2106A
    Elabela(19-32) TFA
    		Agonist 98.78%
    Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.
    Elabela(19-32) TFA
  • HY-P2106
    Elabela(19-32)
    		Agonist 99.64%
    Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.
    Elabela(19-32)
  • 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.
    MM 54
  • HY-P1066
    Apelin-17(human, bovine)
    		Agonist 98.29%
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
    Apelin-17(human, bovine)
  • HY-P2537
    Apelin-12
    		Inhibitor 99.90%
    Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a high affinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect.
    Apelin-12
  • HY-P1064
    Apelin-36(human)
    		Agonist 98.05%
    Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
    Apelin-36(human)
  • 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.
    ALX 40-4C Trifluoroacetate
  • HY-P3162A
    (Ala13)-Apelin-13 TFA
    		Antagonist 99.25%
    (Ala13)-Apelin-13 TFA is a potent apelin receptors (APJ) antagonist. (Ala13)-Apelin-13 TFA inhibits gastric motility through vagal cholinergic pathway.
    (Ala13)-Apelin-13 TFA
  • 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.
    ELA-21 (human)