GHSR Antagonist

LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC₅₀ of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection.

JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R_1a) antagonist with an IC₅₀ of 32 nM.

YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC₅₀ values of 7.90 and 8.27, respectively.

S1H, a mimetic of hGH, is a human growth hormone receptor (hGHR) antagonist. S1H inhibits the interaction of hGH with hGHR. S1H inhibits phosphorylation of STAT5 in cells co-treated with hGH.

YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC₅₀ values of 7.90 and 8.27, respectively.

JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R_1a) antagonist with an IC₅₀ of 32±3 nM in LLC-PK₁ cells.

Cortistatin-8 (CST-8; PCFWKTCK), a neuropeptide, is a GHS-R1a antagonist by counteracting the response of ghrelin on gastric acid secretion. Cortistatin-8 can modulate GH release from somatotroph cells. Cortistatin-8 is a synthetic CST-analogue devoid of any binding affinity to SST-R but capable to bind the GHS-R1a. Cortistatin-8 can exert antagonistic effects on ghrelin actions either in vitro or in vivo in animals.

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.

Acetyl-(D-Arg2)-GRF (1-29) amide (human) is an antagonist of growth hormone releasing factor (GRF). Acetyl-(D-Arg2)-GRF (1-29) amide (human) inhibits the release of growth hormone (GH) and can be used for endocrine research.

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.

AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC₅₀=0.77 nM).

K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (K_i 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.

K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC₅₀=3.4 nM, K_i=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity.

Tezusomant is a growth hormone receptor antagonist. Tezusomant is promising for research on diseases caused by excessive growth hormone secretion, such as acromegaly.

JMV 3008 is a GHS-R1a antagonist with an IC₅₀ of 5.6 nM. JMV 3008 can be used in the research of diseases such as diabetes and obesity.

KwFwLL-NH2, a hexapeptide, is a ghrelin receptor ligand. KwFwLL-NH2 can act as a specific inverse agonist at the ghrelin receptor but with moderate potency (EC₅₀=45.6 nM).