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LY404039

LY404039

产品编号 T6022   CAS 635318-11-5
别名: pomaglumetad

LY404039 (pomaglumetad) 是可口服的mGluR2和mGluR3选择性激动剂,有抗精神病和抗焦虑的作用。它对重组人mGluR2和mGluR3的Ki 分别为 149 和 92 nM,比对其他受体/转运蛋白的抑制性高 100 倍以上。

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LY404039 Chemical Structure
LY404039, CAS 635318-11-5
规格 价格/CNY 货期 数量
1 mg ¥ 185 现货
5 mg ¥ 413 现货
10 mg ¥ 745 现货
25 mg ¥ 1,490 现货
50 mg ¥ 2,380 现货
100 mg ¥ 3,580 现货
1 mL * 10 mM (in DMSO) ¥ 426 现货
产品目录号及名称: LY404039 (T6022)
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纯度: 99.03%
纯度: 99.03%
纯度: 99%
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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 LY404039 (pomaglumetad) is an effective agonist of recombinant human mGlu2(Ki =149 nM)/mGlu3(Ki =92 nM).
靶点活性 mGlu3 (human recombinant):92 nM(Ki), mGlu2 (human recombinant):149 nM(Ki), mGlu2/3 (rat neurons):88 nM(Ki)
体内活性 LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis. [1] In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice. [2] LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior. [3] Moreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex. [4]
激酶实验 Immunoblotting assay of histone acetylation: PANC-1 cells are treated with 2 μg/mL of Scriptaid for 18 h in culture medium. Treated and untreated cells are harvested with trypsin-EDTA, washed with PBS, and resuspended in a protein sample buffer. Protein concentration is determined by BCA protein assay reagents. Fifty μg of proteins from each sample is loaded on a 12% denaturing polyacrylamide gel. Proteins are subsequently transferred to a nylon membrane using MilliblotGraphite Electroblotter I. The nylon membrane is incubated with rabbit antihuman acetyl-lysine antibody, followed by goat antirabbit antibody coupled to horseradish peroxidase, developed with SuperSignal substrates, and detected by film.
别名 pomaglumetad
分子量 235.22
分子式 C7H9NO6S
CAS No. 635318-11-5

存储

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

溶解度

DMSO: Slightly soluble

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Rorick-Kehn LM et al. J Pharmacol Exp Ther, 2007, 321(1), 308-317. 2. Fell MJ et al. J Pharmacol Exp Ther, 2008, 326(1), 209-217. 3. Rodd ZA et al. Behav Brain Res, 2006, 171(2), 207-215. 4. Rorick-Kehn LM et al. Psychopharmacology (Berl), 2007, 193(1), 121-136.
Budesonide Fluocinonide Relacorilant AL 082D06 Glucagon (1-29), bovine, human, porcine hydrochloride Osilodrostat AZD9977 Cortodoxone

相关化合物库

该产品包含在如下化合物库中:
ReFRAME 相关化合物库 已知活性化合物库 经典已知活性库 内分泌激素分子库 神经信号分子库 GPCR靶点分子库 神经递质受体化合物库 谷氨酰胺代谢化合物库 核受体化合物库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
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。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LY404039 635318-11-5 Endocrinology/Hormones Neuroscience Glucocorticoid Receptor GluR inhibit Metabotropic glutamate receptors mGluR cAMP LY-404039 pomaglumetad mGlu3 L-glutamate mGlu2 Inhibitor LY 404039 anxiolytic antipsychotic inhibitor

 

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