ghsr

TC-G-1008 (GPR39-C3) is a zinc receptor agonist with EC50 values of 0.4 nM for rat GPR39 and 0.8 nM for human GPR39.

Emoghrelin, extracted from Heshouwu (Polygonum multiflorum), promotes the secretion of growth hormone by activating the ghrelin receptor [1].

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

Relamorelin(BIM28131, RM131) is a selective and potent ghrelin growth hormone secretagogue receptor (GHSR) agonist with high affinity for GHS-1a receptor (Ki value is 0.42 ± 0.063 nM). Relamorelin(BIM28131, RM131) is also a centrally permeable pentapeptide analog that can increase growth hormone levels and accelerate gastric emptying, and has the potential to study cachexia.

NF-56-EJ40 hydrochloride is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 hydrochloride has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.

Anamorelin (ONO-7643) is a novel ghrelin receptor agonist (EC50: 0.74 nM in the FLIPR assay).

Ibutamoren Mesylate (MK-0677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

TM-N1324 is a GPR39 agonist. TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies to murine GPR39 with EC50s of 180 nM and 5 nM, respectively.

Human growth hormone-releasing factor acetate is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary[1].

Cortistatin-8 acetate is a corticosteroid analog, a GHS-R antagonist with inhibitory effects on the growth hormone pro-secretin receptor.Cortistatin-8 acetate is a synthetic corticosteroid-derived ligand for the growth hormone-releasing peptide receptor and does not alter the endocrine response to acylated growth hormone-releasing peptide or hesperidin in humans.Cortistatin-8 acetate is a synthetic corticosteroid-derived ligand for the growth hormone-releasing peptide receptor.

PF-5190457 is an effective and selective ghrelin receptor inverse agonist (pKi: 8.36).

AnaMorelin hydrochloride (RC-1291 hydrochloride) is a novel ghrelin receptor agonist(EC50 : 0.74 nM, in the FLIPR assay).

Obestatin (rat) acetate is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin (rat) acetate has anti-inflammatory, anti-myocardial infarction and antioxidant properties. Obestatin (rat) acetate suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain.

Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).

hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 nM).

JMV 2959 hydrochloride (925238-89-7 free base) is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.

YIL 781 is a selective ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM), showing a weak affinity for kinesin receptors (K = 6 μM). YIL 781 improves glucose homeostasis in vivo and in vitro by blocking ghrelin secretion.

CJC-1295 acetate(863288-34-0 free base) (DAC:GRF acetate) is a synthetic analogue of growth hormone-releasing hormone (GHRH) (also known as growth hormone-releasing factor (GRF)) and a growth hormone secretagogue (GHS)

KwFwLL-NH2 is a hexapeptide that serves as a ligand for the ghrelin receptor (ghrelin receptor). This compound acts as a specific inverse agonist for the ghrelin receptor, exhibiting moderate potency (EC50=45.6 nM).

SM-130,686 is a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue. It has around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release.

Tabimorelin is a potent, orally-active agonist of the ghrelin/growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue.

EX-1314 (BMS-604992) is a growth hormone secretagogue receptor (GHSR) agonist.

BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule agonist of the growth hormone secretagogue receptor (GHSR). It exhibits high-affinity binding (k i = 2.3 nM) and potent functional activity (EC 50 = 0.4 nM). Additionally, BMS-604992 dihydrochloride stimulates food intake in rodents.

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric intestinal dysmobility disorders [4] [5].