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 (56):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P7061A
    ALX 40-4C Trifluoroacetate
    		Inhibitor 99.78%
    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-P2537
    Apelin-12
    		Inhibitor 99.83%
    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-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-P2197
    ELA-11(human)
    		Agonist 99.54%
    ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pKi of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment.
    ELA-11(human)
  • HY-167712
    (2R,3S)-Azelaprag
    		Agonist 99.10%
    (2R,3S)-Azelaprag ((2R,3S)-AMG 986) (Example 238.0) is a precursor of an apelin receptor agonist (EC50=12 nM) and an isomer of Azelaprag (HY-109111).
    (2R,3S)-Azelaprag
  • HY-P2249
    ELA-21 (human)
    		Agonist 99.97%
    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)
  • HY-P5392A
    Apelin-16, human, bovine acetate
    		99.77%
    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).
    Apelin-16, human, bovine acetate
  • 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.
    ELA-32(human)
  • HY-P1064A
    Apelin-36(human) TFA
    		Agonist 99.42%
    Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
    Apelin-36(human) TFA
  • HY-P7061
    ALX 40-4C
    		Inhibitor
    ALX 40-4C 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
  • HY-21796
    1-Methyl-3-phenylpropylamine
    		99.71%
    ELA-32(human) is a potent critical cardiac developmental peptide that acts through the G-protein–coupled apelin receptor.
    1-Methyl-3-phenylpropylamine
  • HY-P5392
    Apelin-16, human, bovine
    Apelin-16, human, bovine 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)
    Apelin-16, human, bovine
  • HY-P2197A
    ELA-11(human) TFA
    		Chemical 99.03%
    ELA-11(human) TFA is a high affinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
    ELA-11(human) TFA
  • HY-170419
    APJ receptor agonist 10
    		Agonist 99.88%
    APJ receptor agonist 10 is an agonist of the APJ Receptor. APJ receptor agonist 10 can be used for research on pulmonary arterial hypertension.
    APJ receptor agonist 10
  • HY-145285
    APJ receptor agonist 5
    		Agonist
    APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease.
    APJ receptor agonist 5
  • 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.
    APJ receptor agonist 3
  • HY-170419A
    APJ receptor agonist 10 free base
    		Agonist 99.27%
    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.
    APJ receptor agonist 10 free base
  • 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.
    Apelin agonist 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.
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)
  • 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.
    APJ receptor agonist 6