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-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-P3596
    GHRF, mouse
    GHRF, mouse, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse stimulates the release and synthesis of growth hormone.
    GHRF, mouse
  • 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-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-157556
    BPP-2
    BPP-2 is a GHSR ligand with an F element. Using 18F isotope labeling BPP-2, a PET probe targeting GHSR can be obtained. The binding affinity Ki of 18F-BPP-2 for GHSR is 274 nM.
    BPP-2
  • 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-P1421A
    Obestatin(human) TFA
    Obestatin(human) TFA is an endogenous peptide derived from the same prepropeptide as ghrelin. Obestatin(human) suppresses food intake and reduce body weight-gain in rats.
    Obestatin(human) 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-14820
    Macimorelin
    		Agonist
    Macimorelin (EP-1572), a GH secretagogue, is an orally active GHSR agonist. Macimorelin stimulates GH release. Macimorelin can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).
    Macimorelin
  • HY-14495B
    BMS-604992 dihydrochloride
    		Agonist
    BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents.
    BMS-604992 dihydrochloride
  • HY-15242
    Capromorelin
    		Activator
    Capromorelin (CP 424391) is a pyrazolinone-piperidine dipeptide. Capromorelin is an orally active and potent growth hormone secretagogue (GHS) (hGHS-R1a Ki=7 nM, rat pituicyte EC50=3 nM).
    Capromorelin
  • HY-113906A
    (αR,8aS)-GSK1614343
    		Control 99.40%
    (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-P3397
    JV-1-36
    		Antagonist
    JV-1-36 is a growth hormone-releasing hormone (GHRH) antagonist. JV-1-36 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
  • HY-P3056
    GHRF, ovine
    GHRF, ovine is a growth hormone-releasing factor. GHRF is a specific mediator for the effects of hypoglycemia upon the release of pituitary growth hormone (GH).
    GHRF, ovine
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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