ghrelin receptor

Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.

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.

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

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.

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

PF-04628935 is a potent antagonist inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. PF-04628935 is orally bioavailable and brain penetrant.

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

ghrelin receptor (GHS-R1a) agonist

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

GSK 894281 is a ghrelin receptor agonist. It may produces myocardial degeneration/necrosis in rats.

Obestatin(rat) TFA is a cpeptide derived from the Ghrelin gene, consisting of 23 amino acids. This compound modulates physiological processes by suppressing food intake, inhibiting jejunal contraction, and reducing body-weight gain. It functions as an endogenous ligand for G-protein coupled receptor 39 (GPR39). Additionally, Obestatin(rat) TFA exhibits anti-inflammatory, anti-myocardial infarction, and antioxidant activities [1] [2].

JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. At 80 μg kg, JMV3002 inhibits hexarelin-stimulated food intake by up to 98% in rats. It does not induce growth hormone release nor inhibit hexarelin-stimulated growth hormone secretion at a dose of 160 μg kg in infant rats.

YIL781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM) with no significant affinity for the motilin receptor (Ki = 6 μM).

Ulimorelin is a ghrelin receptor agonist (EC50: 29 nM and a Ki of 16 nM). Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors.

TZP-102 is a potent, oral, ghrelin receptor agonist that has been shown to improve diabetic gastroparesis symptoms.

Des-Gln14-Ghrelin TFA serves as a potent endogenous ligand for the growth hormone secretagogue receptor, effectively inducing increases in intracellular calcium levels ([Ca2+]i) in CHO-GHSR62 cells with an EC50 of 2.4 nM.

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

Capromorelin, a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki value of 7 nM for hGHS-R1a and EC50 value of 3 nM for rat pituicyte. Capromorelin

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate ([D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P acetate (96736-12-8 free base)) is a broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.

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].

ghrelin receptor antagonist

High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

orally active ghrelin receptor (GHS-R1a) agonist

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).