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

GHSR

Growth hormone secretagogue receptor

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 (37):

Cat. No. Product Name Effect Purity
  • HY-14734
    Anamorelin
    Agonist 99.86%
    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 98.42%
    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-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-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-U00433A
    JMV 2959 hydrochloride
    Antagonist 98.09%
    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-P3594
    [His1,Nle27] GHRF (1-32), amide, human
    [His1,Nle27] GHRF (1-32), amide, human is a Growth hormone releasing hormone (GHRH) analog. [His1,Nle27] GHRF (1-32), amide, human has great receptor affinity for GHRHR.
  • HY-P3595
    GHRF, porcine
    GHRF, porcine is a growth hormone releasing factor (GHRF) peptide (porcine). GHRF binds to GHSR and induces the release of growth hormone.
  • HY-P3607
    GHRF, bovine
    Activator
    GHRF, bovine (bGRF(1-44)-NH2) is the bovine growth hormone (GH)-releasing factor (GHRF). GHRF, bovine increases the release of bovine GH, and shows a synergistic effect with Hydrocortisone (HY-N0583).
  • HY-12584
    PF-5190457
    Inhibitor 98.78%
    PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
  • 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-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-U00433
    JMV 2959
    Antagonist 99.91%
    JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
  • HY-19884B
    Relamorelin TFA
    Agonist 99.81%
    Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.
  • 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-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-P0231
    AZP-531
    98.76%
    AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
  • HY-13964A
    YIL781 hydrochloride
    Antagonist ≥99.0%
    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-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-19884
    Relamorelin
    Agonist
    Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.
  • HY-19884A
    Relamorelin acetate
    Agonist
    Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.