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-P1155
    GRF (1-29) amide (rat)
    		Inducer 99.80%
    GRF (1-29) amide (rat) is a synthetic peptide which can stimulate the growth hormone (GH) secretion.
    GRF (1-29) amide (rat)
  • 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-P1421
    Obestatin(human)
    		Inhibitor 99.74%
    Obestatin(human) is a 23-amino acid amidated peptide that regulates appetite and gastrointestinal motility via its interaction with GPR39. Obestatin(human) can be used for weight loss. Obestatin(human) cannot penetrate the cell membrane.
    Obestatin(human)
  • HY-50760
    L-692585
    		Agonist 98.94%
    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-N12348
    Emoghrelin
    		Activator
    Emoghrelin, isolated from? Heshouwu Polygonum multiflorum, stimulates growth hormone secretion via activation of the ghrelin receptor.
    Emoghrelin
  • HY-116625
    PF-04628935
    		Antagonist 99.58%
    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-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-113906A
    (αR,8aS)-GSK1614343
    		Control 99.72%
    (αR,8aS)-GSK1614343 is the isomer of GSK1614343 (HY-113906). GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors.
    (αR,8aS)-GSK1614343
  • HY-P3596A
    GHRF, mouse TFA
    		Agonist 98.87%
    GHRF, mouse TFA, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse TFA stimulates the release and synthesis of growth hormone.
    GHRF, mouse TFA
  • HY-P1547
    Somatostatin-25
    		Inhibitor
    Somatostatin-25 is a endogenous neuropeptide hormone that shows inhibitory activity against secretion of growth hormone.
    Somatostatin-25
  • 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-P4405
    (D-Ala2)-GRF (1-29) amide (human)
    		Agonist 98.83%
    (D-Ala2)-GRF (1-29) amide (human) is a superagonist of GRF, exhibiting extremely high GH-releasing activity about 50 times that of GRF (1-29) in both pigs and rats.
    (D-Ala2)-GRF (1-29) amide (human)
  • 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-176995
    AZ-GHS-38
    		Agonist
    AZ-GHS-38 (compound 38) is an orally active CNS-penetrant inverse agonist of growth hormone secretagogue receptor (GHS-R1a) with an IC50 of 6.7 nM. AZ-GHS-38 results in acute reduction of food intake in wild-type mice. AZ-GHS-38 can be used for anti-obesity research.
    AZ-GHS-38
  • 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-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-118995
    L-739943
    		Activator
    L-739943 is a potent, and orally active growth hormone (GH) secretagogue with an ED50 of 1 nM. L-739943 stimulates GH release in beagle dogs. L-739943 can be used for GH-related diseases research.
    L-739943
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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