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ADX88178 {[allProObj[0].p_purity_real_show]}

货号:A710732 Ambeed 开学季,买赠积分,赢豪礼

ADX88178是一种代谢型谷氨酸受体 4 (mGluR4) 的正变构调节剂,作用于人 mGluR4 的 EC50 为 4 nM。该化合物适用于研究神经系统疾病,特别是在神经退行性疾病的治疗中有潜在的应用价值。

ADX88178 化学结构 CAS号:1235318-89-4
ADX88178 化学结构
CAS号:1235318-89-4
ADX88178 3D分子结构
CAS号:1235318-89-4
ADX88178 化学结构 CAS号:1235318-89-4
ADX88178 3D分子结构 CAS号:1235318-89-4
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ADX88178 纯度/质量文件 产品仅供科研

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ADX88178 生物活性

描述 ADX88178 is a highly potent and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 4 (mGluR4), serving as a novel radioligand for mGluR4 imaging. It enhances glutamate-induced activation of human mGluR4 with EC50 values as low as 4 nM, showing negligible effects on other mGluR subtypes (EC50 > 30 μM), which underlines its specificity[1]. Furthermore, ADX88178 demonstrates brain penetrance and selectivity as a positive allosteric modulator of mGluR4. In studies involving microglia pre-treated with ADX88178 or LAP4 before exposure to LPS, both treatments significantly reduce TNFα levels, indicating their anti-inflammatory potential. Remarkably, even a minimal concentration of 1 nM ADX88178 is effective in suppressing TNFα production, maintaining its efficacy at higher concentrations of 10 and 100 nM. This suggests ADX88178's potent anti-inflammatory action at remarkably low doses[2].
体内研究

Administered orally, ADX88178 demonstrates a dose-responsive enhancement in exploratory behavior in mice, evident by increased open-arm entries in the elevated plus maze (EPM) test. Specifically, doses of 3, 10, and 30 mg/kg of ADX88178 result in 5-, 7-, and nearly 13-fold surges in open-arm entries, respectively, in comparison to those given the vehicle control. Similarly, the time mice spend in the open arms escalates dose-dependently; at doses of 3, 10, and 30 mg/kg, there are increases of 8-, 12-, and 24-fold, respectively, relative to the vehicle controls. In rats, oral doses of ADX88178 ranging from 10 to 100 mg/kg also show a dose-dependent elevation in the EPM test's open-arm entries. At concentrations of 10, 30, and 100 mg/kg, the increases are 5-, 8-, and more than 10-fold, respectively, compared with vehicle-treated counterparts. Additionally, the duration spent in the open arms by rats rises in a dose-dependent manner; with 10, 30, and 100 mg/kg doses leading to 7.5-, 11-, and 13-fold increases, respectively, when juxtaposed with the controls. This behavior indicates a significant anxiolytic effect of ADX88178 in rodent models, improving their exploratory behavior and reducing anxiety-like symptoms as the dosage increases[3].

体外研究

ADX88178 is a highly potent and selective positive allosteric modulator of the metabotropic glutamate receptor subtype 4 (mGluR4), serving as a novel radioligand for mGluR4 imaging. It enhances glutamate-induced activation of human mGluR4 with EC50 values as low as 4 nM, showing negligible effects on other mGluR subtypes (EC50 > 30 μM), which underlines its specificity[1].

Furthermore, ADX88178 demonstrates brain penetrance and selectivity as a positive allosteric modulator of mGluR4. In studies involving microglia pre-treated with ADX88178 or LAP4 before exposure to LPS, both treatments significantly reduce TNFα levels, indicating their anti-inflammatory potential. Remarkably, even a minimal concentration of 1 nM ADX88178 is effective in suppressing TNFα production, maintaining its efficacy at higher concentrations of 10 and 100 nM. This suggests ADX88178's potent anti-inflammatory action at remarkably low doses[2].

ADX88178 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 L

[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.

ADX88178 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.67mL

0.73mL

0.37mL

18.36mL

3.67mL

1.84mL

36.72mL

7.34mL

3.67mL

ADX88178 技术信息

CAS号1235318-89-4
分子式C12H12N6S
分子量 272.329
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 16 mg/mL(58.75 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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