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ADX88178

产品编号 T4500 CAS 1235318-89-4

ADX88178 是一种代谢型谷氨酸受体 4 (mGluR4) 正变构调节剂，对人 mGluR4 的 EC50 为 4 nM。

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ADX88178, CAS 1235318-89-4

规格	价格/CNY	货期
1 mg	￥ 398	现货
2 mg	￥ 569	现货
5 mg	￥ 913	现货
10 mg	￥ 1,490	现货
25 mg	￥ 2,520	现货
50 mg	￥ 3,760	现货
100 mg	￥ 5,380	现货
1 mL * 10 mM (in DMSO)	￥ 971	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.
靶点活性	mGluR4 (human):4 nM(EC50)
体外活性	ADX88178 is used as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). ADX88178 potentiates glutamate-mediated activation of human mGluR4 with EC50 values of 4 nM without significant effects on other mGluRs (EC50 > 30 μM). Microglia are pretreated with 1, 10 or 100 nM ADX88178 or 100 nM LAP4 for 30 min followed by LPS treatment for 24 h prior to collecting culture supernatant for ELISA measurement of TNFα levels. The pre-treatment with ADX88178 and LAP4 both significantly attenuate LPS-induced TNFα levels. As little as 1 nM of ADX88178 is sufficient to inhibit TNFα, and is as effective at concentrations of 10 and 100 nM.
体内活性	In rats, ADX88178 (10-100 mg/kg p.o.) dose-dependently increases the number of open-arm entries in the rat EPM test. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 5-, 8-, and more than 10-fold increases in the number of open-arm entries, respectively, when compared with the vehicle-treated controls. Also, ADX88178 dose-dependently increases the time spent in the open arms. Specifically, at 10, 30, and 100 mg/kg ADX88178, there are 7.5-, 11-, and 13-fold increases in time spent in the open arms when compared with the vehicle-treated controls.
激酶实验	Stability of UAMC00039 in RPMI medium or assay buffer (50 mM cacodylate buffer pH5.5) is monitored at 37 °C. The inhibitors' capacity (IC50) to inhibit DPPII is measured at different time points (up to 48 h). U937 cells are incubated with various concentrations of UAMC00039 for 15 min at 37 °C in RPMI. Cells are then ished with PBS, lysed and assayed for DPPII activity. Concentration–response and time–response curves are generated from incubations of PBMC with UAMC00039 (0.01 nM–1 μM) in RPMI at 37 °C for 1, 5, 15, 30 and 60 min. Ished cells are lysed overnight at 4 °C using 100 mM HEPES buffer pH 7.4, 10 mM EDTA, 70 μg/mL aprotinin and 1% octylglucoside.
细胞实验	ADX88178 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. After adhesion to the chamber slides, microglia from WT and mGlu4 KO microglia pre-treated with 1 nM, 10 nM, 100 nM ADX88178, or 100 nM L-AP4. Each treatment is performed in quadruplicate. Thirty minutes after treatment with ADX88178 or L-AP4, 100 ng/mL LPS is added to the cultures and the cells are incubated at 37 °C for an additional 24 h. At the end of the 24 h treatment period, media is collected and analyzed for TNFα, and the cells are for iNOS and MHC II expression by immunocytochemistry.
动物实验	Mice and Rat Male mice (n=8-10/group) are treated orally (p.o.) via gavage with vehicle [1% carboxymethyl cellulose (CMC)], ADX88178 (1, 3, 10 and 30 mg/kg) or Diazepam (1.5 mg/kg). Male rats (n=10/group) are treated p.o. with vehicle (1% CMC), ADX88178 (10, 30, and 100 mg/kg), or Diazepam (3 mg/kg). After 60 minutes, animals are individually placed in the center of the maze (facing one of the closed arms) and left to explore for 5 minutes. A terminal blood sample is collected from all ADX88178-treated animals at the end of the experiment, and plasma is analyzed for the pharmacokinetic studies. The number of open-arm and closed-arm entries, as well as the time (seconds) spent in the open arms of the maze, is analyzed by one-way analysis of variance followed by Dunnett's test.

分子量	272.33
分子式	C12H12N6S
CAS No.	1235318-89-4

存储

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

溶解度

DMSO: 50 mg/mL

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配液计算器

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参考文献

1. Fujinaga M, et al. Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4). Bioorg Med Chem Lett. 2016 Jan 15;26(2):370-4. 2. Ponnazhagan R, et al. The Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator ADX88178 Inhibits Inflammatory Responses in Primary Microglia. J Neuroimmune Pharmacol. 2016 Jun;11(2):231-7. 3. Kalinichev M, et al. Characterization of the novel positive allosteric modulator of the metabotropic glutamate receptor 4 ADX88178 in rodent models of neuropsychiatric disorders. J Pharmacol Exp Ther. 2014 Sep;350(3):495-505.

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

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μL

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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。

% DMSO+

% +

% Tween 80+

% ddH₂O

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计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

ADX88178 1235318-89-4 Neuroscience GluR Inhibitor mGluR Metabotropic glutamate receptors inhibit ADX 88178 ADX-88178 inhibitor

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ADX88178

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