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 99.64%
    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-10199A
    Ibutamoren
    		Agonist
    Ibutamoren (MK-677) is an orally active growth hormone secretagogue receptor (GHSR) agonist and a nonpeptide growth hormone secretagogue. Ibutamoren can be used for metabolic research.
    Ibutamoren
  • 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-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-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-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-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-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
  • HY-50760
    L-692585
    		Agonist 99.32%
    L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
    L-692585
  • HY-13964
    YIL781
    		Antagonist 99.68%
    YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
    YIL781
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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