For research use only. Not for therapeutic Use.
YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively[1][2][3][4].
YIL781 (10-300 nM) induces a concentration-dependent parallel rightward shift of the ghrelin CRC with a slight but statistically significant depression of the maximal response at 100 and 300 nM, reaching a similar agonist maximal response of approximately 90%[3].
YIL781 (0.1 to 5 μg/5 μl) attenuates ghrelin-induced up-regulation of the blood glucose level. The
i.t. treatment with YIL781 alone does not affect the blood glucose level (F = 0.8160; P = 0.5095)[4].
| Catalog Number | I012025 |
| CAS Number | 1640226-17-0 |
| Synonyms | 6-(4-fluorophenoxy)-2-methyl-3-[[(3S)-1-propan-2-ylpiperidin-3-yl]methyl]quinazolin-4-one;hydrochloride |
| Molecular Formula | C24H29ClFN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H28FN3O2.ClH/c1-16(2)27-12-4-5-18(14-27)15-28-17(3)26-23-11-10-21(13-22(23)24(28)29)30-20-8-6-19(25)7-9-20;/h6-11,13,16,18H,4-5,12,14-15H2,1-3H3;1H/t18-;/m0./s1 |
| InChIKey | QQGRMONBDBMLSP-FERBBOLQSA-N |
| SMILES | CC1=NC2=C(C=C(C=C2)OC3=CC=C(C=C3)F)C(=O)N1CC4CCCN(C4)C(C)C.Cl |
| Reference | [1]. William P Esler, et al. Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss Endocrinology. 2007 Nov;148(11):5175-85. [2]. Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530. [3]. Elisabetta Perdonà, et al. Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors. Eur J Pharmacol. 2011 Jan 10;650(1):178-83. [4]. Yun-Beom Sim, et al. Ghrelin administered spinally increases the blood glucose level in mice. Peptides. 2014 Apr;54:162-5. |
