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ADX88178

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Chemical Structure| 1235318-89-4 同义名 : -
CAS号 : 1235318-89-4
货号 : A710732
分子式 : C12H12N6S
纯度 : 99%+
分子量 : 272.329
MDL号 : MFCD21340285
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：
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].
实验方案
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
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.