- Signaling Pathways
- GPCR/G Protein
- 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.
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Apelin Receptor (APJ) Related Products (57)
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Azelaprag
0 ImagesSynonyms: AMG 986Azelaprag (Example 263.0) is a candidate active molecule for an Apelin receptor agonist with an EC50 of 0.32 nM for the apelin receptor. -
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[Pyr1]-Apelin-13
0 ImagesSynonyms: [pGlu1]-Apelin-13[Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist. -
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Apelin-13 TFA
0 ImagesCat. No.: HY-P1944AApelin-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. -
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ML221
0 ImagesML221 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. -
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ML339
0 ImagesML339 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. -
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YL-GB063
0 ImagesCat. No.: HY-181540YL-GB063 is an Apelin receptor (APJ) antagonist. YL-GB063 inhibits Apelin-induced APJ β-arrestin recruitment (IC50 of 3.1 μM in HTLA cells). YL-GB063 has anti-cancer activity against ovarian cancer. -
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Anti-APLNR Antibody
0 ImagesCat. No.: HY-P991861 -
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B-007
0 ImagesCat. No.: HY-183777B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure. -
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BMS-986224
0 ImagesBMS-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. -
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Apelin-13
0 ImagesApelin-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. -
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CMF019
0 ImagesCMF019 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. -
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MM 07
0 ImagesMM 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. -
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- Apelin-17(human, bovine)
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Apelin-36(human)
0 ImagesApelin-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. -
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MM 54
0 ImagesMM 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. -
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Elabela(19-32)
0 ImagesElabela(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. -
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- (Ala13)-Apelin-13 TFA
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Apelin-36(rat, mouse)
0 ImagesApelin-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. -
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ELA-32(human) TFA
0 ImagesCat. No.: HY-P2196APurity: 99.93%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. -
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ML233
0 ImagesML233 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). -
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