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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
[His1,Nle27] GHRF (1-32), amide, human 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.
AZ-GHS-22 V75382 AZ-GHS-22 1143020-91-0 AZ-GHS-22 is a potent, non-CNS penetrating GHS-R1a inverse agonist (IC50=0.77 nM).
BMS-604992 dihydrochloride (EX-1314 dihydrochloride) 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.
BMS-604992 free base (EX-1314 free base) 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.
BPP-2 V84190 BPP-2
Cortistatin-8 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.
des-Gln14-Ghrelin V75369 des-Gln14-Ghrelin 293735-04-3 des-Gln14-Ghrelin is the second endogenous ligand of the growth hormone secretagogue receptor.
des-Gln14-Ghrelin TFA V79084 des-Gln14-Ghrelin TFA des-Gln14-Ghrelin TFA is the second endogenous ligand of the growth hormone secretagogue receptor.
Emoghrelin V75366 Emoghrelin 928262-58-2 Emoghrelin is extracted from Polygonum multiflorum and stimulates the secretion of growth hormone through activation of ghrelin receptors.
Ghrelin receptor full agonist-2 V75374 Ghrelin receptor full agonist-2 2602452-73-1 Ghrelin receptor full agonist-2 is a effective Ghrelin receptor agonist (activator).
GSK1614343 V75380 GSK1614343 1092076-04-4 GSK1614343 is a potent antagonist of the growth hormone secretagogue type 1a (GHS1a) receptor.
Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA; Somatorelin (1-44) amide (human) (TFA)) 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.
Ibutamoren Mesylate (Ibutamoren Mesylate; MK-677; MK-0677) 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).
JMV 2959 hydrochloride 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.
JMV 3002 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.
K-(D-1-Nal)-FwLL-NH2 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).
K-(D-1-Nal)-FwLL-NH2 TFA 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).
L-692585 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.
Obestatin(rat) TFA 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.
PF-5190457 V4451 PF-5190457 1334782-79-4 PF-5190457 is a novel, potent, orally available and selective ghrelin receptor inverse agonist with a pKi of 8.36.
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