growth hormone secretagogue receptor

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.

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.

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.

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

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

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.

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).

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.

KARI 201 is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. Additionally, KARI 201 acts as an agonist of the growth hormone secretagogue receptor (ghrelin receptor). It is capable of improving the neuropathological characteristics of Alzheimer's disease.

Ghrelin receptor full agonist-3 (Compound 22) is a selective, potent, orally active full agonist of the growth hormone secretagogue receptor (ghrelin receptor) with an EC50 value of 1.8 nM. It stimulates pulsatile secretion of growth hormone (GH), significantly increasing both the frequency and duration of GH release, thereby inducing a sustained rise in insulin-like growth factor-1 (IGF-1) levels. This compound is applicable for research in oncology and chronic obstructive pulmonary disease.

AZ-GHS-38 (compound 38) is an orally active inverse agonist of the growth hormone secretagogue receptor (GHS-R1a) that can cross the blood-brain barrier, with an IC50 of 6.7 nM. It has been shown to acutely reduce food intake in wild-type mice and may be used for anti-obesity research.

(S)-PF-5190457 ((S)-PF-05190457) is the S-enantiomer of PF-5190457. PF-5190457 (PF-05190457) acts as an effective and selective inverse agonist of the growth hormone secretagogue receptor (ghrelin receptor), with a pKi of 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

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.

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

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.