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LY3027788 hydrochloride

产品编号 T38790 CAS 1377615-55-8

LY3027788 hydrochloride is a diester analog of LY3020371, a selective antagonist of the metabotropic glutamate 2 and 3 receptors (mGlu2/3). It serves as a highly potent and orally bioavailable prodrug of LY3020371. Notably, LY3027788 hydrochloride exhibits antidepressant efficacy.

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LY3027788 hydrochloride Chemical Structure

LY3027788 hydrochloride, CAS 1377615-55-8

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		6-8周

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其他形式的 LY3027788 hydrochloride:

LY3027788
询价

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	LY3027788 hydrochloride is a diester analog of LY3020371, a selective antagonist of the metabotropic glutamate 2 and 3 receptors (mGlu2/3). It serves as a highly potent and orally bioavailable prodrug of LY3020371. Notably, LY3027788 hydrochloride exhibits antidepressant efficacy.
体外活性	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].
体内活性	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 ED 60 was 8.2 mg/kg.

分子量	628.03
分子式	C25H32ClF2NO11S
CAS No.	1377615-55-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Witkin JM, et, al. Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression. J Pharmacol Exp Ther. 2017 Apr;361(1):68-86. 2. Witkin JM, et, al. mGlu2/3 receptor antagonism: A mechanism to induce rapid antidepressant effects without ketamine-associated side-effects. Pharmacol Biochem Behav. 2020 Mar;190:172854.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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