875258-85-8

875258-85-8 structure

Name: YIL-781
Chemical Name: 6-(4-Fluorophenoxy)-3-{[(3S)-1-isopropyl-3-piperidinyl]methyl}-2- methyl-4(3H)-quinazolinone hydrochloride (1:1)
CAS Number: 875258-85-8
Molecular Formula: C₂₄H₂₈FN₃O₂
Molecular Weight: 409.50
Create Date: 2016-04-29 03:45:15
Modify Date: 2024-01-02 11:14:21
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].

Name	6-(4-Fluorophenoxy)-3-{[(3S)-1-isopropyl-3-piperidinyl]methyl}-2- methyl-4(3H)-quinazolinone hydrochloride (1:1)
Synonyms	Mesulergine hydrochloride YIL-781

Description	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].
Related Catalog	Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> GHSR
In Vitro	YIL781 (10-300 nM) 诱导生长素释放肽 CRC 的浓度依赖性平行右移，在 100 和 300 nM 时最大反应有轻微但具有统计学意义的抑制，达到约 90% 的类似激动剂最大反应[3]。
In Vivo	YIL781 (0.1-5 μg/5 μL) 减弱生长素释放肽诱导的血糖水平上调。而单独使用 YIL781 不会影响血糖水平[4]。
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. [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.