產(chǎn)品目錄

規(guī)格	10mg 50mg
CAS	885104-09-6
別名
化學(xué)名	(S)-1-(5-bromopyrimidin-2-yl)-N-(2,4-dichlorobenzyl)pyrrolidin-3-amine hydrochloride
分子式	C15H15BrCl2N4.HCl
分子量	438.58
溶解度	<8.77mg/ml in DMSO
儲(chǔ)存條件	Desiccate at RT
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LY2389575 is described here instead of LY2389575 hydrochloride. LY2389575 is a selective negative allosteric modulator (NAM) of metabotropic glutamate receptor 3 (mGlu3) with an IC50 value of 4.2 μM [1].

The metabotropic glutamate receptors (mGlus) are members of the GPCR family C. They are characterized by a large extracellular amino-terminal domain for binding agonist. Eight mGlus had been found and were assigned to three groups based on their pharmacology, sequence homology, and mechanisms to couple to effector. They are Group I: mGlu1 and mGlu5; Group II: mGlu2 and mGlu3; Group III: mGlu4,6,7,8 [1].

In mixed neuronal cultures, LY2389575 abolished the protective activity of 1 μM LY379268 (the orthosteric mGlu2/3 receptor agonist) in the concentration range of 0.1 to 1 μM and amplified Aβ toxicity on its own at the highest concentration. In the absence of Aβ, LY2389575 at these concentrations was not toxic (numbers of dead neurons in control cultures and in cultures treated with 1 μM LY2389575 were 41 ± 3, and 42 ± 1, respectively). Further data indicated that LY2389575 was able to amplify Aβ toxicity and abolish the neuroprotective activity of LY379268 only in cultures containing wild-type astrocytes. In the FLIPR assay system, LY2389575 behaved as a noncompetitive mGlu3 receptor antagonist with an efficacy of 100 ± 0.68% and an IC50 value of 190 ± 26 nM. LY2389575 failed in affecting responses mediated by all other mGlu receptor subtypes or GABAB receptors [2].

No in vivo data for the application of this drug had been found.

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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