YIL781

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].

Product Specifications

CAS Number

[875258-85-8]

UNSPSC

12352005

Target

GHSR

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/yil781.html

Purity

99.68

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C[C@@H]2CN(C(C)C)CCC2)C(C)=NC3=C1C=C(OC4=CC=C(F)C=C4)C=C3

Molecular Formula

C24H28FN3O2

Molecular Weight

409.50

References & Citations

[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.