YIL-781

Modify Date: 2025-08-25 14:42:35

YIL-781 Structure
YIL-781 structure
Common Name YIL-781
CAS Number 875258-85-8 Molecular Weight 409.50
Density N/A Boiling Point N/A
Molecular Formula C24H28FN3O2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of YIL-781


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].

 Names

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

 YIL-781 Biological Activity

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
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.  

 Chemical & Physical Properties

Molecular Formula C24H28FN3O2
Molecular Weight 409.50
Exact Mass 445.19300
PSA 47.36000
LogP 5.49660

 Synonyms

Mesulergine hydrochloride
YIL-781
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