2. Vías de señalización
  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.

Productos relacionados con Apelin Receptor (APJ) (56):

Cat. No. Nombre del producto Efecto Pureza Chemical Structure
  • HY-175818
    APJ antagonist-1
    		Antagonist
    APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC50 of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis.
    APJ antagonist-1
  • HY-160076
    APJ receptor agonist 8
    		Agonist 99.60%
    APJ receptor agonist 8 (compound 99) is an agonist of APJ receptor. APJ receptor agonist 8 increases the load independent cardiac contractility of isolated perfused rat hearts.
    APJ receptor agonist 8
  • 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-178982
    Apelin agonist 2
    		Agonist
    Apelin agonist 2 (Compound 35) is an orally active APLNR agonist. Apelin agonist 2 can significantly inhibit the accumulation of cAMP (EC50 = 10 nM). Apelin agonist 2 exhibits a significant improvement in glucose tolerance. Apelin agonist 2 can be used to study metabolic diseases such as diabetes.
    Apelin agonist 2
  • 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-139486
    AM-8123
    		Agonist 99.89%
    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-P2250
    ELA RR>GG
    		Control
    ELA RR>GG (ELA-32 negative control), an ELABELA (ELA-32 human) mutant peptide, is inactive. ELA RR>GG is a negative control for ELABELA (HY-P2196).
    ELA RR>GG
  • 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-P992190
    Anti-Apelin Antibody
    Anti-Apelin Antibody is a monoclonal antibody that targets apelin. It can be used in ELISA, FACS, and functional assays. For isotype controls of anti-Apelin Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Apelin Antibody
  • HY-103254R
    ML221 (Standard)
    		Antagonist
    ML221 (Standard) is the analytical standard of ML221 (HY-103254). This product is intended for research and analytical applications. 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 (Standard)
  • 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-169752
    APJ receptor agonist 11
    		Agonist
    APJ receptor agonist 11 (Ex 174) is a APJ receptor agonist with IC50 values ranging from 0.01 nM to 10 nM. APJ receptor agonist 11 can be used in the study of cardiovascular diseases.
    APJ receptor agonist 11
  • HY-103080R
    CMF019 (Standard)
    		Agonist
    CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. 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 (Standard)