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 (26):

Cat. No. Product Name Effect Purity
  • HY-P1944A
    Apelin-13 TFA
    		≥98.0%
    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.
  • HY-103254
    ML221
    		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.
  • HY-P1033
    [Pyr1]-Apelin-13
    		99.69%
    [Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.
  • HY-P2106A
    Elabela(19-32) TFA
    		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.
  • HY-P2196A
    ELA-32(human) TFA
    		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.
  • 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.
  • HY-P2106
    Elabela(19-32)
    		98.05%
    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.
  • HY-103080
    CMF019
    		99.05%
    CMF019 is a 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.
  • HY-P2271
    MM 54
    		99.21%
    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.
  • HY-108003
    MM 07
    		98.08%
    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.
  • HY-109111
    Azelaprag
    		99.84%
    Azelaprag (Example 263.0) is an apelin receptor agonist agent candidate.
  • HY-P2249
    ELA-21 (human)
    		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.
  • HY-P1944
    Apelin-13
    Apelin-13 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 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome.
  • HY-139876
    APJ receptor agonist 3
    APJ receptor agonist 3 is a potent and orally active APJ receptor agonist with an EC50 value of 0.027 nM.
  • HY-126293
    Apelin agonist 1
    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.
  • HY-P3346
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)
    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.
  • HY-P2196
    ELA-32(human)
    ELA-32 (human) is a potent critical cardiac developmental peptide that acts through the G-protein–coupled apelin receptor.
  • 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.
  • HY-145284
    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.
  • HY-P2197
    ELA-11(human)
    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.