YIL-781

Names

[ Name ]:
YIL-781

[Synonym ]:
Mesulergine hydrochloride
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]:

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₈FN₃O₂

[ Molecular Weight ]:
409.50

[ Exact Mass ]:
445.19300

[ PSA ]:
47.36000

[ LogP ]:
5.49660

MSDS

Click to get detail MSDS

Related Compounds

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