1. Signaling Pathways
  2. GPCR/G Protein
  3. GHSR

GHSR

GHSR (Growth hormone secretagogue receptor) is a seven transmembrane G protein-coupled receptor with high expression in the anterior pituitary, pancreatic islets, thyroid gland, heart and various regions of the brain. Two types of GHS-R are accepted to be present, GHS-R1a and GHS-R1b.

Ghrelin is a gastric polypeptide displaying strong GH-releasing activity by activation of the GHS-R1a located in the hypothalamus-pituitary axis. GHS-R1a is a G-protein-coupled receptor that, upon the binding of ghrelin or synthetic peptidyl and non-peptidyl ghrelin-mimetic agents known as GHS, preferentially couples to Gq, ultimately leading to increased intracellular calcium content. Beside the potent GH-releasing action, ghrelin and GHS influence food intake, gut motility, sleep, memory and behavior, glucose and lipid metabolism, cardiovascular performances, cell proliferation, immunological responses and reproduction.

GHSR Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-14734
    Anamorelin Agonist 99.62%
    Anamorelin (RC-1291) is a potent ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
  • HY-50844
    Ibutamoren Mesylate Agonist
    Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.
  • HY-103007
    TC-G-1008 Agonist 99.03%
    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-14734A
    Anamorelin hydrochloride Agonist 99.97%
    Anamorelin (RC-1291) hydrochloride is a potent ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
  • HY-U00433A
    JMV 2959 hydrochloride Antagonist 98.07%
    JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
  • HY-19884A
    Relamorelin acetate Agonist
    Relamorelin (RM-131) acetate, a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin acetate can promote food intake and adiposity in mice. Relamorelin acetate can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders.
  • HY-14495A
    BMS-604992 free base Agonist
    BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents.
  • HY-13964A
    YIL781 hydrochloride Antagonist
    YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
  • HY-108699
    TM-N1324 Agonist 99.88%
    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-15243
    Capromorelin Tartrate Agonist 98.71%
    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
  • HY-12584
    PF-5190457 Inhibitor ≥98.0%
    PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  • HY-10957
    L-692429 Agonist 99.88%
    L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.
  • HY-P0231
    AZP-531
    AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
  • HY-P0089
    Human growth hormone-releasing factor
    Human growth hormone-releasing factor (Growth Hormone Releasing Factor human) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.
  • HY-P0089A
    Human growth hormone-releasing factor TFA 98.22%
    Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.
  • 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.
  • HY-14903
    Ulimorelin Agonist
    Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
  • HY-P1306
    Obestatin(rat)
    Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
  • HY-14495
    BMS-604992 Agonist
    BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents.
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2 Antagonist
    K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity.
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