ghs-r1a

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.

JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a) (IC50: 32 nM).

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.

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.

GHSR-1a agonist-1 (Compound 4b) is an orally active agonist of the human growth hormone secretagogue receptor 1a (GHSR-1a) with an EC50 of 0.49 nM. It effectively stimulates the release of endogenous growth hormone by activating GHSR-1a. Doses as low as 0.1 mg/kg (administered orally) can increase body weight and length in 4-week-old rats. GHSR-1a agonist-1 is applicable in research on pediatric growth and developmental delays.

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

ghrelin receptor (GHS-R1a) agonist

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.

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].

LEAP-2 acetate (Human liver expressed antimicrobial peptide-2) is an endogenous antagonist of the ghrelin receptor GHS-R1a with an IC50 of 6.0 nM, suppressing the orexigenic effects of ghrelin, attenuating ghrelin-induced growth hormone release, reducing basal food intake. LEAP-2 acetateexhibit direct antimicrobial activity against model microorganisms, thereby serving as a multifunctional peptide for mechanistic studies of obesity, metabolism, and infection biology.

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

orally active ghrelin receptor (GHS-R1a) agonist

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

AZ-GHS-22 is an inverse agonist of the growth hormone secretagogue receptor 1a (GHS-R1a), which is also known as the ghrelin receptor.1It binds to GHS-R1a with an IC50value of 0.77 nM. AZ-GHS-22 decreases food intake in mice by 54% in the first two hours after administration of a 100 mg/kg dose. 1.McCoull, W., Barton, P., Brown, A.J.H., et al.Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonistsJ. Med. Chem.57(14)6128-6140(2014)

LEAP-2 (Human liver expressed antimicrobial peptide-2) is an antimicrobial peptide and an endogenous competitive antagonist of growth hormone-releasing peptide, as well as a reverse agonist of constitutive GHS-R1a activity, used for research on obesity and other metabolic diseases.

An endogenous ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing of the rat ghrelin gene. Potently induces Ca2+ release in cells expressing ghrelin receptors (EC50 = 2.4 nM) and stimulates GH release in vivo.