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-P4405
    (D-Ala2)-GRF (1-29) amide (human)
    		Agonist
    (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-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
  • HY-P10673
    KwFwLL-NH2
    		Antagonist
    KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC50=45.6 nM).
    KwFwLL-NH2
Cat. No. Product Name / Synonyms Application Reactivity
GHSR Isoform Comparison

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