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LY3020371

产品编号 T38791 CAS 1377615-75-2

LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.

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LY3020371, CAS 1377615-75-2

规格	价格/CNY		货期	数量
25 mg	待询		6-8周

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其他形式的 LY3020371:

LY3020371 hydrochloride
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	LY3020371 is a highly potent and selective antagonist targeting the glutamate (mGlu) 2/3 receptor, showcasing excellent inhibition at Ki values of 5.26 nM and 2.50 nM for hmGluR2 and hmGluR3, respectively. With its remarkable affinity and specificity, LY3020371 serves as a valuable tool in depression research.
靶点活性	mGluR3 (human):2.50 nM (Ki), mGluR2 (human):5.26 nM (Ki)
体外活性	LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [ 3 H]-459477 with high affinity[1]. LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC 50 =16.2 nM) and mGlu3 (IC 50 =6.21 nM) receptors[1]. LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation[1]. LY3020371 (1-10000 nM) reverses LY379268-suppressed, K + -evoked glutamate release, with an IC 50 of 86 nM[1]. LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC 50 of 33.9 nM[1].
体内活性	LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats[2]. LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats[2]. LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats[2]. LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence[2]. LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay[2]. Animal Model: Male Sprague-Dawley rats (230-350 g)[1]Dosage: 0.3, 1, 3 mg/kg Administration: I.v. daily 5 days per week for 2 weeks Result: Increased the number of actively firing dopamine neurons in the VTA of anesthetized rats.

分子量	359.34
分子式	C15H15F2NO5S
CAS No.	1377615-75-2

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, In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu 2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. 2. 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.

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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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