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-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-P4750
    Acetyl-(D-Arg2)-GRF (1-29) amide (human)
    		Antagonist 99.67%
    Acetyl-(D-Arg2)-GRF (1-29) amide (human) is an antagonist of growth hormone releasing factor (GRF). Acetyl-(D-Arg2)-GRF (1-29) amide (human) inhibits the release of growth hormone (GH) and can be used for endocrine research.
    Acetyl-(D-Arg2)-GRF (1-29) amide (human)
  • 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
  • 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.
    Ulimorelin
  • HY-P3397A
    JV-1-36 acetate
    		Antagonist 99.27%
    JV-1-36 acetate is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 acetate inhibits the production of reactive oxygen species in A549 lung cancer cells. JV-1-36 can be used to study the effect of GHRH antagonists in vitro .
    JV-1-36 acetate
  • 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.
    Human growth hormone-releasing factor
  • 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.
    Relamorelin
  • 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.
    Relamorelin acetate
  • 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-145364
    Ghrelin receptor full agonist-2
    		Agonist
    Ghrelin receptor full agonist-2 (compound 12j) is a highly potent Ghrelin receptor full agonist.
    Ghrelin receptor full agonist-2
  • HY-115272
    GSK894490A
    		Agonist
    GSK894490A is a non-peptide ghrelin receptor agonist.
    GSK894490A
  • HY-116625
    PF-04628935
    		Antagonist
    PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research.
    PF-04628935
  • HY-113906
    GSK1614343
    		Antagonist
    GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models.
    GSK1614343
  • 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.
    [His1,Nle27] GHRF (1-32), amide, human
  • 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.
    BMS-604992 free base
  • HY-153095
    PF-6870961
    		Agonist
    PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.
    PF-6870961
  • HY-P10283
    S1H
    		Antagonist
    S1H, a mimetic of hGH, is a human growth hormone receptor (hGHR) antagonist. S1H inhibits the interaction of hGH with hGHR. S1H inhibits phosphorylation of STAT5 in cells co-treated with hGH.
    S1H
  • HY-P1306
    Obestatin(rat)
    		98.73%
    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.
    Obestatin(rat)
  • HY-137061
    AZ-GHS-22
    		Antagonist
    AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM).
    AZ-GHS-22
  • 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.
    GHRF, porcine
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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