Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents[1].
[His1,Nle27] GHRF (1-32), amide, human is a Growth hormone releasing hormone (GHRH) analog. [His1,Nle27] GHRF (1-32), amide, human has great receptor affinity for GHRHR[1].
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM)[1].
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[1].
GSK894490A is a non-peptide ghrelin receptor agonist[1].
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents[1].
GHRF, porcine is a growth hormone releasing factor (GHRF) peptide (porcine). GHRF binds to GHSR and induces the release of growth hormone[1][2].
Anamorelin hydrochloride is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
Alexamorelin is a new synthetic heptapeptide which inhibits GHS binding in vitro.
Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release[1][2].
AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research[1][2].
Emoghrelin, isolated from? Heshouwu Polygonum multiflorum, stimulates growth hormone secretion via activation of the ghrelin receptor[1].
Macimorelin (EP-1572), a GH secretagogue, is an orally active GHSR agonist. Macimorelin stimulates GH release. Macimorelin can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS)[1][2][3].
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities[1][2].
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition[1][2][3].
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer drug and also a selective agonist of GPR132.
Relamorelin (RM-131) acetate, a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin acetate can promote food intake and adiposity in mice. Relamorelin acetate can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3].
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models[1].
Examorelin, a synthetic growth hormone-releasing peptide, has been proven to possess cardioprotective actions through its binding to the growth hormone secretagogue receptor (GHSR) 1a and the non-GHSR receptor CD36.
Relamorelin (RM-131), a Ghrelin analog, is a potent ghrelin receptor agonist, with a Ki of 0.42 nM for GHS-1a. Relamorelin can promote food intake and adiposity in mice. Relamorelin can be used for the research of cachexia, gastroparesis, and gastric/intestinal dysmobility disorders[1][2][3].
Anamorelin is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.