| Bioactivity | YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively[1][2][3][4]. | ||||||||||||
| Invitro | YIL-781 (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 | ||||||||||||
| In Vivo | YIL781 (0.1 至 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]。 | ||||||||||||
| Name | YIL781 | ||||||||||||
| CAS | 875258-85-8 | ||||||||||||
| Formula | C24H28FN3O2 | ||||||||||||
| Molar Mass | 409.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |