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LY3027788 hydrochloride
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。
LY3027788 hydrochloride图片
CAS NO:1377615-55-8

LY3027788 hydrochloride 是 LY3020371 的二酯类似物,是mGlu2/3 receptor的拮抗剂,是 LY3020371 的一种有效的口服活性前药。LY3027788 hydrochloride 具有抗抑郁功效。
生物活性

LY3027788 hydrochloride, a diester analog of LY3020371 which is anmGlu2/3 receptorantagonist, is a potent and orally active prodrug of LY3020371. LY3027788 hydrochloride has antidepressant efficacy[1][2].

IC50& Target[1]

mGluR2

 

mGluR3

 

体外研究
(In Vitro)

LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1].
LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1].
LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1].
LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].

体内研究
(In Vivo)

LY3027788 (4.8-27 mg/kg; a single p.o.) produces antidepressant-like decreases in immobility times in the forced-swim test in mice[1].
LY3027788 (4.8-16 mg/kg; a single p.o.) enhances the locomotor stimulant effects of quinpirole at the dose of 16 mg/kg in the locomotor activity assay in mice[1].
LY3027788 (10-30 mg/kg; a single p.o.) dose dependently increases the wake time of rats without engendering rebound hypersomnolence[1].
LY3027788 (a single p.o.) leads to the rapid and dose-proportionate appearance of the pharmacologically active species LY3020371 in plasma of both mouse (4.8-27 mg/kg) and rat (3-30 mg/kg)[1].

Animal Model:Male Sprague-Dawley mice (20-25 g)[1]
Dosage:4.8, 16, 27 mg/kg
Administration:A single p.o. (60 minutes prior to testing)
Result:Potent and efficacious with a minimal effective dose of 16 mg/kg in the mouse forced-swim assay.
The ED60was 8.2 mg/kg.
分子量

628.04

Formula

C25H32ClF2NO11S

CAS 号

1377615-55-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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