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 (39):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P1944
    Apelin-13
    		Agonist
    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.
    Apelin-13
  • 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-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-125976
    ML233
    		Agonist ≥98.0%
    ML233 is a non-peptide based potent apelin receptor (APJ) agonist (EC50=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor (>79 μM).
    ML233
  • HY-P1065
    Apelin-36(rat, mouse)
    		Agonist 98.07%
    Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) 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) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
    Apelin-36(rat, mouse)
  • 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-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
  • 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.
    (Ala13)-Apelin-13
  • HY-P1064A
    Apelin-36(human) TFA
    		Agonist
    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-145284
    APJ receptor agonist 4
    		Agonist
    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.
    APJ receptor agonist 4
  • HY-P1065A
    Apelin-36(rat, mouse) TFA
    		Agonist
    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-36(rat, mouse) TFA
  • HY-P1066A
    Apelin-17(human, bovine) TFA
    		Agonist
    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.
    Apelin-17(human, bovine) TFA
  • HY-P2197
    ELA-11(human)
    		Agonist 99.03%
    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-139486
    AM-8123
    		Agonist
    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.
    AM-8123
  • HY-P3347
    NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
    		Agonist
    NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=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.
    NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
  • HY-133036
    APJ receptor agonist 1
    		Agonist
    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.
    APJ receptor agonist 1
  • 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