GHSR

GHSR

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.

GHSR related products

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.
V4686 Anamorelin 249921-19-5 Anamorelin (formerly also known as RC-1291 and ONO-7643) is a novel, potent, and orally bioavailable ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
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.
V2145 Capromorelin 193273-66-4 Capromorelin, also known as CP-424,391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM).
V16403 Capromorelin tartrate (CP-424,391) 193273-69-7 Capromorelin, formerly known as CP-424,391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM).
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.
V4077 Ibutamoren mesylate 59752-10-0 Ibutamoren mesylate (formerly also known as MK-677, MK-0667, and L-163,191) is a novel, non-peptide, potent, long-acting, orally-active, and selective agonist of the ghrelin receptor and a growth hormone secretagogue (GHSR), mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin.
V75365 Ibutamoren Mesylate (Ibutamoren Mesylate; MK-677; MK-0677) 159752-10-0 Ibutamoren Mesylate (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.
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).
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.
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