貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S82521-1mg	99.9%	￥230.00 S82521-1mg ￥230.00 現(xiàn)貨	10 10	-	-	-
S82521-5mg	99.9%	￥540.00 S82521-5mg ￥540.00 現(xiàn)貨	11 >10	-	-	-
S82521-10mg	99.9%	￥890.00 S82521-10mg ￥890.00 現(xiàn)貨	10 10	-	-	-
S82521-50mg	99.9%	￥2200.00 S82521-50mg ￥2200.00 現(xiàn)貨	2 2	-	-	-
S82521-100mg	≥98%	￥3200.00 S82521-100mg ￥3200.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.

產(chǎn)品描述：

ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.

靶點(diǎn)：

mGluR4:4 nM (EC50);GluR

體外研究：

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

體內(nèi)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

參考文獻(xiàn)：

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):370-374. 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. [Content Brief] 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.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.672 ml	18.36 ml	36.72 ml
5 mM	0.734 ml	3.672 ml	7.344 ml
10 mM	0.367 ml	1.836 ml	3.672 ml
50 mM	0.073 ml	0.367 ml	0.734 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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ADX88178

2-PyriMidinaMine,4-Methyl-N-[5-Methyl-4-(1H-pyrazol-4-yl)-2-thiazolyl]-