产品
编 号:F197645
分子式:C24H29ClFN3O2
分子量:445.96
产品类型
结构图
CAS No: 1640226-17-0
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产品详情
生物活性:
YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
体内研究:
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。Animal Model:Conscious mice.
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).
体外研究:
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。