secretagogue

Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

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.

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.

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).

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

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.

Repaglinide D5 is deuterium labeled Repaglinide. Repaglinide is an insulin secretagogue for treatment type-2 diabetes mellitus.

Ibutamoren (MK-677) is a drug which acts as a potent, orally active growth hormone secretagogue, mimicking the GH stimulating action of the endogenous hormone ghrelin. It also alters the metabolism of body fat and so may have an application in the treatment of obesity.

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.

Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, specifically targets vimentin to facilitate Par-4 secretion. It also induces lysosomal membrane permeabilization (LMP) and promotes non-apoptotic cell death in cancer cells [1].

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

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.

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.

BMS-317180 is a potent, novel, orally effective growth hormone secretagogue (GHS) that shows an excellent safety profile in preclinical studies. The compound was advanced into clinical development.

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

L 163255 is a type of growth hormone secretagogue (GHS).

L-739943 is a growth hormone secretagogue.

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.

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)

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.