| DC7357 |
Anamorelin
Featured
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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. |
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| DC11246 |
Ghrelin agonist HM01
Featured
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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. |
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| DC7020 |
Ibutamoren mesylate
Featured
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Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| DC44099 |
Capromorelin tartrate
Featured
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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. |
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| 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. |
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| 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. |
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| DC48404 |
Ghrelin receptor full agonist-2 |
Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist. |
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| DC49032 |
AZ-GHS-22 |
AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM). |
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| 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. |
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| DC70536 |
KARI 201
Featured
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KARI-201 is a multifunctional small molecule that demonstrates dual activity as a highly selective inhibitor of acid sphingomyelinase (ASM) and an agonist of the ghrelin receptor. It operates as a competitive inhibitor by binding directly to the active site of ASM. Studies reveal that the incorporation of KARI-201 into ASM decreases in a concentration-dependent manner with sphingomyelin, resulting in KM values of 332.5, 433.9, and 572.6 μM at KARI-201 concentrations of 1, 10, and 100 μM, respectively. In preclinical models, KARI-201 has shown efficacy in reducing amyloid pathology and reversing cognitive deficits in APP/PS1 mice. Additionally, it enhances autophagy degradation by promoting lysosomal biogenesis in neuronal cells. As a ghrelin receptor agonist, KARI-201 also supports hippocampal neurogenesis and improves synaptic plasticity, making it a promising therapeutic candidate for neurodegenerative conditions. |
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| DC70634 |
N8279
Featured
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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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| DC72820 |
Macimorelin acetate |
Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS). |
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