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

GHSR

Growth hormone secretagogue receptor; Ghrelin receptor

GHSR

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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 Isoform Specific Products:

GHSR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14734
    Anamorelin
    		Agonist 99.94%
    Anamorelin (RC-1291) is a potent ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
    Anamorelin
  • HY-50844
    Ibutamoren Mesylate
    		Agonist 99.86%
    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.
    Ibutamoren Mesylate
  • HY-103007
    TC-G-1008
    		Agonist 99.61%
    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.
    TC-G-1008
  • HY-12584
    PF-5190457
    		Inhibitor 98.34%
    PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
    PF-5190457
  • 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.
    Anamorelin hydrochloride
  • HY-P1139
    Cortistatin-8
    		Antagonist
    Cortistatin-8 (CST-8; PCFWKTCK), a neuropeptide, is a GHS-R1a antagonist by counteracting the response of ghrelin on gastric acid secretion. Cortistatin-8 can modulate GH release from somatotroph cells. Cortistatin-8 is a synthetic CST-analogue devoid of any binding affinity to SST-R but capable to bind the GHS-R1a. Cortistatin-8 can exert antagonistic effects on ghrelin actions either in vitro or in vivo in animals.
    Cortistatin-8
  • HY-117584
    L-163255 free base
    L-163255 free base is an orally active spiropiperidine GH secretagogue. L-163255 (free base) can also increase plasma IGF-I level.
    L-163255 free base
  • HY-10957A
    L-692429 hydrochloride
    		Agonist
    L-692429 (MK-0751) hydrochloride is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 hydrochloride binds to G protein-coupled receptor with a Ki of 63 nM.
    L-692429 hydrochloride
  • HY-108699
    TM-N1324
    		Agonist 99.91%
    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.
    TM-N1324
  • HY-13964A
    YIL781 hydrochloride
    		Antagonist 99.48%
    YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
    YIL781 hydrochloride
  • 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.
    JMV 2959
  • HY-P1366
    des-​Gln14-​Ghrelin
    		98.61%
    des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
    des-​Gln14-​Ghrelin
  • HY-19884B
    Relamorelin TFA
    		Agonist 99.89%
    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.
    Relamorelin TFA
  • HY-P3304
    MR 409
    		Agonist 99.51%
    MR 409 is a selected growth hormone-releasing hormone (GHRH) agonist. MR 409 has remarkable neuroprotective effects through enhancing endogenous neurogenesis in cerebral ischemic mice. MR 409 also inhibits the in vivo growth of lung cancer.
    MR 409
  • HY-P1155
    GRF (1-29) amide (rat)
    		Inducer 99.94%
    GRF (1-29) amide (rat) is a synthetic peptide which can stimulate the growth hormone (GH) secretion.
    GRF (1-29) amide (rat)
  • HY-10957
    L-692429
    		Agonist 99.90%
    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.
    L-692429
  • HY-P0231
    AZP-531
    		98.54%
    AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
    AZP-531
  • HY-P0089A
    Human growth hormone-releasing factor TFA
    		99.66%
    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.
    Human growth hormone-releasing factor TFA
  • 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.
    JMV 2959 hydrochloride
  • HY-15243
    Capromorelin Tartrate
    		Agonist 98.19%
    Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
    Capromorelin Tartrate
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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