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Apelin receptor

The apelin receptor (also known as the APJ receptor) is a G protein-coupled receptor which binds apelin and Apela/ELABELA/Toddler.

  • CMF019
    T108431586787-08-7In house
    CMF019 is a potent agonist of the Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ (pKis: 8.58, 8.49, and 8.71 for the human, rat, and mouse).
    • $122
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  • ALX 40-4C acetate
    TP1364L
    ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).
    • $221
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  • ELA-14(human) acetate
    TP1923L1
    ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide.
    • $95
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  • ELA-11 (human) acetate(1784687-32-6 free base)
    TP1922L1
    ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
    • $133
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  • Apelin-12 acetate
    T39823L
    Apelin-12 acetate possesses a high affinity to orphan receptor APJ receptor. Apelin-12 acetate inhibits the JNK and p38 MAPK signaling pathway of the apoptosis-related MAPKs family, thus offering protection to neurons.
    • $228
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  • (2R,3S)-Azelaprag
    T14390L2049979-31-7In house
    (2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.
    • $195
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  • AM-8123
    T394422049973-02-4In house
    AM-8123 is an orally available nonpeptide APJ agonist.AM-8123 reduces collagen load and improves cardiac function. AM-8123 ameliorates myocardial infarction in rats and can be used to study cardiovascular diseases such as heart failure.
    • $293 TargetMol
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  • Azelaprag
    T143902049980-18-7In house
    Azelaprag (AMG 986) is an effective small-molecule apelin receptor agonist. Azelaprag can be used to treat neurological diseases and cardiovascular diseases.
    • $396
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  • [Pyr1]-Apelin-13
    TP1260217082-60-5
    [Pyr1]-Apelin-13 ([pGlu1]-Apelin-13) is a potent and selective endogenous Apelin receptor (APJ) agonist.
    • $89
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    TargetMol | Citations Cited
  • ML221
    T4390877636-42-5
    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.
    • $50
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    TargetMol | Citations Cited
  • (Ala13)-Apelin-13 acetate
    T35374L
    (Ala13)-Apelin-13 acetate, an APJ antagonist, modulates CRF-induced enhanced colonic motility, visceral sensation, and gut barrier.
    • $118
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    TargetMol | Inhibitor Sale
  • BMS-986224
    T394482055200-88-7
    BMS-986224 is an orally active, potent, and selective APJ receptor agonist. BMS-986224 has the potential to study heart failure.
    • $399
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