Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| M30023 | Macimorelin | Macimorelin (EP-1572), a GH secretagogue, is an orally active GHSR agonist. Macimorelin stimulates GH release. Macimorelin can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS). |
| M29841 | Relamorelin TFA | Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research. |
| M28907 | Relamorelin acetate | Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a Ki of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research. |
| M28758 | YIL781 hydrochloride | YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively. |
| M28320 | K-(D-1-Nal)-FwLL-NH2 | K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity. |
| M27840 | TM-N1324 | TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39. |
| M27838 | AZ-GHS-22 | AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM). |
| M27777 | (αR,8aS)-GSK1614343 | (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06. |
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