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-14820A
    Macimorelin acetate
    		Agonist 98.96%
    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-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-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
    		Antagonist 99.40%
    (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06.
    (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-14734R
    Anamorelin (Standard)
    		Agonist
    Anamorelin (Standard) is the analytical standard of Anamorelin. This product is intended for research and analytical applications. Anamorelin (RC-1291) is a potent ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
    Anamorelin (Standard)
  • HY-111232
    GSK894281
    		Agonist
    GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research.
    GSK894281
  • HY-129207
    JMV 3002
    Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg/kg.
    JMV 3002
  • HY-14734B
    Anamorelin Fumarate
    		Agonist
    Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
    Anamorelin Fumarate
  • HY-N12348
    Emoghrelin
    		Activator
    Emoghrelin, isolated from? Heshouwu Polygonum multiflorum, stimulates growth hormone secretion via activation of the ghrelin receptor.
    Emoghrelin
  • HY-116959
    SM-130686
    SM-130686 is an oxindole derivative and an active GH secretagogue (GHS). SM-130686 stimulates GH release with a Half-maximum stimulation of 6.3 nM. SM-130686 has an orally active.
    SM-130686
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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