产品
编 号：F085319
分子式：C12H12N6S
分子量：272.33
分子式：C12H12N6S
分子量：272.33
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 1235318-89-4
产品详情
生物活性：
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
体内研究：
In mice, ADX88178 (1-30 mg/kg p.o.) dose-dependently increases the number of open-arm entries. Specifically, at 3, 10, and 30 mg/kg ADX88178, there are 5-, 7-, and almost 13-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 3, 10, and 30 mg/kgADX88178, there are 8-, 12-, and 24-fold increases in the time spent in the open arms when compared with the vehicle-treated controls. 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.
体外研究：
ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. 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). ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4.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.
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
体内研究：
In mice, ADX88178 (1-30 mg/kg p.o.) dose-dependently increases the number of open-arm entries. Specifically, at 3, 10, and 30 mg/kg ADX88178, there are 5-, 7-, and almost 13-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 3, 10, and 30 mg/kgADX88178, there are 8-, 12-, and 24-fold increases in the time spent in the open arms when compared with the vehicle-treated controls. 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.
体外研究：
ADX88178 is developed as a potent and selective mGluR4 positive allosteric modulator. 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). ADX88178 is novel potent, selective, and brain-penetrant positive allosteric modulator of the mGlu4.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.
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