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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-145364
    Ghrelin receptor full agonist-2
    		Agonist
    Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.
    Ghrelin receptor full agonist-2
  • 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-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-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
  • HY-14820A
    Macimorelin acetate
    		Agonist
    Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).
    Macimorelin acetate
  • HY-14495
    BMS-604992
    		Agonist
    BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents.
    BMS-604992
  • HY-P1366A
    des-​Gln14-​Ghrelin TFA
    des-Gln14-Ghrelin TFA 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 TFA
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA
    		Antagonist
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
    K-(D-1-Nal)-FwLL-NH2 TFA
  • HY-153095A
    PF-6870961 hydrochloride
    		Agonist
    PF-6870961 hydrochloride 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 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.
    PF-6870961 hydrochloride
  • 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).
    GHRF, bovine
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2
    		Antagonist
    K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity.
    K-(D-1-Nal)-FwLL-NH2
  • HY-P1306A
    Obestatin(rat) TFA
    Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA 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) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
    Obestatin(rat) TFA
  • 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