YIL781 hydrochloride

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1640226-17-0

YIL781 hydrochloride 是有效的、具有口服活性的胃促生长素受体(GHSR)的拮抗剂。YIL781 hydrochloride 可改善大鼠体内葡萄糖稳态。YIL781 hydrochloride 可抑制饥饿素诱导的钙反应，pIC₅₀值分别为 7.90 和 8.27。

生物活性

YIL781 hydrochloride is a potent and orally activeghrelin receptor (GHSR)antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL-781 hydrochloride inhibits the calcium response induced by ghrelin with pIC₅₀values of 7.90 and 8.27, respectively^[1]^[2]^[3]^[4].

体外研究
(In Vitro)

YIL-781 (10-300 nM) induces a concentration-dependent parallel rightward shift of the ghrelin CRC with a slight but statistically significant depression of the maximal response at 100 and 300 nM, reaching a similar agonist maximal response of approximately 90%^[3].

体内研究
(In Vivo)

YIL781 (0.1 to 5 μg/5 μl) attenuates ghrelin-induced up-regulation of the blood glucose level. The i.t. treatment with YIL781 alone does not affect the blood glucose level (F = 0.8160; P = 0.5095)^[4].

Animal Model:	Conscious mice^[4].
Dosage:	0.1 to 5 μg/5 μl.
Administration:	Intrathecal (i.t.) injection.
Result:	Attenuated ghrelin-induced up-regulation of the blood glucose level (F = 0.7506; P = 0.5729) (YIL781 5 g + ghrelin 5 g –9.1% at 30 min; –14.9% at 60 min). The i.t. treatment with YIL781 alone did not affect the blood glucose level (F = 0.8160; P = 0.5095).

分子量

445.96

性状

Solid

Formula

C₂₄H₂₉ClFN₃O₂

CAS 号

1640226-17-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)