| 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. |
| DC44099 |
Capromorelin tartrate
|
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. |
| 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. |
| 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). |
| 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. |
| 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. |
| DC49032 |
AZ-GHS-22
|
AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM). |
| DC48404 |
Ghrelin receptor full agonist-2
|
Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist. |
