875258-85-8
875258-85-8
Chemical Structure
YIL781
- CAS No.: 875258-85-8
- Formula:C24H28FN3O2
- Molecular Weight:409.50
IUPAC Name: (S)-6-(4-fluorophenoxy)-3-((1-isopropylpiperidin-3-yl)methyl)-2-methylquinazolin-4(3H)-one
InChIKey: FRKXOBMDEXCHHD-SFHVURJKSA-N
SMILES: O=C1N(C[C@@H]2CN(C(C)C)CCC2)C(C)=NC3=C1C=C(OC4=CC=C(F)C=C4)C=C3
Biological Activity: YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively[1][2][3][4].
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YIL781 | 99.68% | YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. Timothy H. Moran, et al. Gut Peptides: Targets for Antiobesity Drug Development? Endocrinology. 2009 Jun; 150(6): 2526–2530. [Content Brief]
- [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. [Content Brief]
- [4]. Yun-Beom Sim, et al. Ghrelin administered spinally increases the blood glucose level in mice. Peptides. 2014 Apr;54:162-5. [Content Brief]
Keywords
