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 |
---|---|---|---|---|
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. | |
V75382 | AZ-GHS-22 | 1143020-91-0 | AZ-GHS-22 is a potent, non-CNS penetrating GHS-R1a inverse agonist (IC50=0.77 nM). | |
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. | |
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. | |
V84190 | BPP-2 | |||
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. | |
V75369 | des-Gln14-Ghrelin | 293735-04-3 | des-Gln14-Ghrelin is the second endogenous ligand of the growth hormone secretagogue receptor. | |
V79084 | des-Gln14-Ghrelin TFA | des-Gln14-Ghrelin TFA is the second endogenous ligand of the growth hormone secretagogue receptor. | ||
V75366 | Emoghrelin | 928262-58-2 | Emoghrelin is extracted from Polygonum multiflorum and stimulates the secretion of growth hormone through activation of ghrelin receptors. | |
V75374 | Ghrelin receptor full agonist-2 | 2602452-73-1 | Ghrelin receptor full agonist-2 is a effective Ghrelin receptor agonist (activator). | |
V75380 | GSK1614343 | 1092076-04-4 | GSK1614343 is a potent antagonist of the growth hormone secretagogue type 1a (GHS1a) receptor. | |
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. | ||
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). | |
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. | |
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. | |
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). | |
V80475 | K-(D-1-Nal)-FwLL-NH2 TFA | K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Kis are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). | ||
V98906 | KwFwLL-NH2 | 942266-38-8 | KwFwLL-NH2 is a hexapeptide that is a ligand for the ghrelin receptor. | |
V75371 | L-692585 | 145455-35-2 | L-692585 is a potent, non-peptidyl growth hormone secretagogue receptor (GHS-R1a) agonist/activator with a Ki of 0.8 nM. | |
V75373 | Obestatin(rat) TFA | 1312186-27-8 | Obestatin(rat) TFA is a bioactive peptide encoded by the Ghrelin gene and consists of 23 amino acid (AA)s. |