The anterior pituitary, pancreatic islets, thyroid gland, heart, and different parts of the brain have high expression levels of the seven transmembrane G protein-coupled receptor known as GHSR (growth hormone secretagogue receptor). GHS-R1a and GHS-R1b are the two types of GHS-R that are recognized as existing.
Gastric polypeptide ghrelin activates the GHS-R1a in the hypothalamus-pituitary axis, where it exhibits strong GH-releasing activity. When ghrelin or artificial peptidyl and non-peptidyl ghrelin-mimetic agents, known as GHS, bind to the GHS-R1a, a G-protein-coupled receptor, it preferentially couples to Gq, ultimately increasing the intracellular calcium content. Ghrelin and GHS also have significant effects on food intake, gut motility, sleep, memory, and behavior in addition to their powerful GH-releasing action. They also affect cardiovascular performance, cell proliferation, immune responses, and reproduction.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V75372 | [His1,Nle27] GHRF (1-32), amide, human | 94034-78-3 | [His1,Nle27] GHRF (1-32), amide, human is a growth hormone-releasing hormone (GHRH) analog. |
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V75382 | AZ-GHS-22 | 1143020-91-0 | AZ-GHS-22 is a potent, non-CNS penetrating GHS-R1a inverse agonist (IC50=0.77 nM). |
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V111585 | AZ-GHS-38 | 1143021-16-2 | AZ-GHS-38 (compound 38) is an orally effective, blood-brain barrier-crossing inverse growth hormone secretagogue receptor (GHS-R1a) agonist with an IC50 value of 6.7 nM. |
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V75375 | BMS-604992 dihydrochloride (EX-1314 dihydrochloride) | 1469750-46-6 | BMS-604992 (EX-1314) di-HCl is a selective, orally bioactive, small molecule growth hormone secretagogue receptor (GHSR) agonist. |
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V75381 | BMS-604992 free base (EX-1314 free base) | 760944-56-7 | BMS-604992 (EX-1314) free base is a selective, orally bioactive, small molecule growth hormone secretagogue receptor (GHSR) agonist. |
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V84190 | BPP-2 | ||
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V86608 | Cortistatin-8 | 485803-62-1 | Cortistatin-8 (CST-8; PCFWKTCK) is a neuropeptide and a GHS-R1a antagonist that counteracts the secretion of ghrelin in response to gastric acid and modulates ghrelin release from somatotrophs in vitro. |
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V116149 | CP-464709 | 193272-70-7 | CP-464709 is an auxin-releasing peptide receptor agonist that can cross the blood-brain barrier. |
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V75369 | des-Gln14-Ghrelin | 293735-04-3 | des-Gln14-Ghrelin is the second endogenous ligand of the growth hormone secretagogue receptor. |
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V79084 | des-Gln14-Ghrelin TFA | des-Gln14-Ghrelin TFA is the second endogenous ligand of the growth hormone secretagogue receptor. | |
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V75366 | Emoghrelin | 928262-58-2 | Emoghrelin is extracted from Polygonum multiflorum and stimulates the secretion of growth hormone through activation of ghrelin receptors. |
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V75374 | Ghrelin receptor full agonist-2 | 2602452-73-1 | Ghrelin receptor full agonist-2 is a effective Ghrelin receptor agonist (activator). |
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V110888 | Ghrelin receptor full agonist-3 | 2243167-93-1 | Auxin-releasing peptide receptor full agonist-3 (compound 22) is a highly selective, potent, and orally effective auxin-releasing peptide receptor full agonist with an EC50 value of 1.8 nM. |
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V120270 | GHRF, mouse TFA | GHRF, also known as mouse growth hormone releasing factor, is a peptide composed of 44 amino acids. | |
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V75380 | GSK1614343 | 1092076-04-4 | GSK1614343 is a potent antagonist of the growth hormone secretagogue type 1a (GHS1a) receptor. |
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V76914 | Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA; Somatorelin (1-44) amide (human) (TFA)) | Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA) is a hypothalamic polypeptide that stimulates the production and release of growth hormone via binding to the growth hormone-releasing hormone receptor (GHRHR) of prepituitary cells. | |
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V75365 | Ibutamoren HCl (Ibutamoren Mesylate; MK-677; MK-0677) | 159752-10-0 | Ibutamoren HCl (MK-677) is a potent, non-peptide agonist of the growth hormone secretagogue receptor (GHSR). |
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V75368 | JMV 2959 hydrochloride | 2448414-54-6 | JMV 2959 HCl is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist that acts on LLC-PK1 cells and inhibits GHS-R1a with IC50 of 32±3 nM. |
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V86609 | JMV 3002 | 925239-03-8 | Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and signals to the hypothalamic regulatory nuclei that control energy homeostasis. |
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V75377 | K-(D-1-Nal)-FwLL-NH2 | 1394288-22-2 | K-(D-1-Nal)-FwLL-NH2 is a high-affinity, potent, inverse ghrelin receptor agonist (activator) (EC50=3.4 nM; Ki=4.9 nM). |