Home > Inhibitors & Agonists > GPCR > Ghrelin Receptor (GHSR)
Cat. No. Product name CAS No.
DC7357 Anamorelin Featured

Anamorelin(RC1291; ONO-7643) is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia.

249921-19-5
DC11246 Ghrelin agonist HM01

Ghrelin agonist HM01 is a novel potent, orally available ghrelin (GHS-R) agonist with Ki of 1.42 nM (human GHS-R1a), induces potent activation of intracellular calcium signaling with EC50 of 1.25 nM.

1394860-28-6
DC7020 Ibutamoren Mesylate(MK-0677) Featured

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.

159752-10-0
DC28975 Ulimorelin

Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.

842131-33-3
DC41146 L-692585

L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.

145455-35-2
DC41753 Obestatin(rat)

Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.

869705-22-6
DC41754 Obestatin(rat) TFA

Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.

DC42494 Human growth hormone-releasing factor TFA

Human growth hormone-releasing factor TFA (Growth Hormone Releasing Factor human TFA) is a hypothalamic polypeptide and stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.

DC44099 Capromorelin tartrate Featured

Capromorelin Tartrate (CP 424391-18), 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 of 7 nM for hGHS-R1a and EC50 of 3 nM for rat pituicyte.

193273-66-4
DC44912 K-(D-1-Nal)-FwLL-NH2

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

1394288-22-2
DC46585 K-(D-1-Nal)-FwLL-NH2 TFA

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

DC48404 Ghrelin receptor full agonist-2

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

2602452-73-1
DC49032 AZ-GHS-22

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

1143020-91-0
DC50225 GSK1614343

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.

1092476-84-0
DC70536 KARI 201

KARI 201 (KARI-201) is a dual-action small molecule that exhibit highly selective inhibition effects on Acid sphingomyelinase (ASM), and act as a ghrelin receptor agonist.KARI 201 is a competitive inhibitor that binds to the active site of ASM.Incorporation of KARI 201 into ASM was decreased with increasing concentrations of sphingomyelin, yielding KM values of 332.5, 433.9, and 572.6 μM at 1, 10, and 100 μM KARI 201, respectively.Administration of KARI 201 reduces amyloid pathology and restores cognitive impairment in APP/PS1 mice.KARI 201 ameliorates defective autophagy degradation by regulating lysosomal biogenesis in neurons.KARI 201 is a ghrelin receptor agonist and improves hippocampal neurogenesis and synapse plasticity.

2376132-22-6
DC70634 N8279

N8279 (NCATS-SM8864) is a selective, brain-penetrant small molecule Gαq-biased GHSR1a agonist with binding IC50 of 1.3 uM.N8279 is nearly an order of magnitude (8.9-fold) more potent than the endogenous ligand ghrelin and is a full agonist.iCa2+ EC50 of N8279 is 41-fold more potent than its GHSR1a binding IC50, suggesting possible allosteric activity, which could be competitively inhibited by GHSR1a antagonists YIL781 and JMV2959.N8279 is a weak activator of GHSR1a-mediated, βarr2-dependent cellular responses relative to ghrelin.N8279 requires receptor sites and/or conformational states driven by the GHSR1a ECD that are distinct from ghrelin.N8279 is brain-penetrant and attenuates aberrant DAergic behavior in mice.

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