1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. LY3027788 hydrochloride

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。

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LY3027788 hydrochloride Chemical Structure

LY3027788 hydrochloride Chemical Structure

CAS No. : 1377615-55-8

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Other Forms of LY3027788 hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY3027788 hydrochloride, a diester analog of LY3020371 which is an mGlu2/3 receptor antagonist, 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ED60 was 8.2 mg/kg.
分子量

628.04

Formula

C25H32ClF2NO11S

CAS 号
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.

纯度 & 产品资料
参考文献

LY3027788 hydrochloride 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
LY3027788 hydrochloride
目录号:
HY-117606A
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