1. GPCR/G Protein
  2. GHSR


GHSR (Growth hormone secretagogue receptor) is a member of the G-protein coupled receptor family. GHSR may play a role in energy homeostasis and regulation of body weight. The pathway activated by binding of ghrelin to the growth hormone secretagogue receptor, GHSR1a, regulates the activation of the downstream mitogen-activated protein kinase, Akt, nitric oxide synthase, and AMPK cascades in different cellular systems. One of the important features of GHSR1a displays constitutive activity possessing basal activity in the absence of an agonist, resulting in a high degree of receptor internalization as well as of signaling activity. Inverse agonists for the ghrelin receptor could be particularly interesting for the treatment of obesity. A range of selective ligands for the GHSR receptor are now available and are being developed for several clinical applications. GHSR agonists have appetite-stimulating and growth hormone-releasing effects, and are likely to be useful for the treatment of muscle wasting and frailty associated with old-age and degenerative diseases. On the other hand, GHSR antagonists have anorectic effects and are likely to be useful for the treatment of obesity.

GHSR Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-14734
    Anamorelin Agonist 99.91%
    Anamorelin is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
  • HY-14734A
    Anamorelin hydrochloride Agonist 99.80%
    Anamorelin hydrochloride is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
  • HY-50844
    Ibutamoren Mesylate Agonist
    Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.
  • HY-P0166
    Alexamorelin Inhibitor 98.93%
    Alexamorelin is a new synthetic heptapeptide which inhibits GHS binding in vitro. Sequence: Ala-His-{Me-Trp}-Ala-Trp-Phe-Lys-NH2.
  • HY-P0169A
    GHRP-2 metabolite 1 Agonist 99.96%
    GHRP-2 metabolite 1 is one of the GHRP-2 metabolites. Growth hormone releasing peptide -2 (GHRP-2), a peptide with six amino acid units (D-Ala-D-beta- + Nal-Ala-Trp-D-Phe-Lys-NH2), is a synthetic agonist of ghrelin. GHRP-2 can significantly promote the release of growth hormone, improving the blood growth hormone concentration in animals and humans. Sequence: .
  • HY-12584
    PF-5190457 Agonist
    PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  • HY-P0166A
    Alexamorelin Met 1 Inhibitor 99.82%
    Alexamorelin Met 1 is one of the metabolites of alexamorelin. The heptapeptide Ala-His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2 (Alexamorelin) is a synthetic molecule which inhibits growth hormone secretagogue binding in vitro. Sequence: .
  • HY-111343
    ONC212 Agonist 99.20%
    ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer drug and also a selective agonist of GPR132.
  • HY-103007
    TC-G-1008 Agonist 99.71%
    TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
  • HY-P0231
    AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. Sequence: Cyclo(Arg-Val-Gln-Ser-Pro-Glu-His-Gln).
  • HY-19235
    Examorelin Activator 99.79%
    Examorelin, a synthetic growth hormone-releasing peptide, has been proven to possess cardioprotective actions through its binding to the growth hormone secretagogue receptor (GHSR) 1a and the non-GHSR receptor CD36.
  • HY-15243
    Capromorelin Tartrate Agonist 98.01%
    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
  • HY-108699
    TM-N1324 Agonist 98.91%
    TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
  • HY-U00433
    JMV 2959 Antagonist
    JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
  • HY-14734B
    Anamorelin Fumarate Agonist
    Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.