货号	规格	价格	上海	北京	珠海	重庆	武汉
S88327-2mg促销	≥99%	￥900.00 ￥150.00 S88327-2mg ￥150.00 现货	9 9	-	-	-	-
S88327-5mg促销	≥99%	￥1600.00 ￥310.00 S88327-5mg ￥310.00 现货	10 10	-	-	-	-
S88327-10mg促销	≥99%	￥2400.00 ￥550.00 S88327-10mg ￥550.00 现货	6 6	-	-	-	-
S88327-25mg促销	≥99%	￥4400.00 ￥790.00 S88327-25mg ￥790.00 现货	9 9	-	-	-	-
S88327-50mg促销	≥99%	￥6800.00 ￥1350.00 S88327-50mg ￥1350.00 现货	4 4	-	-	-	-
S88327-100mg促销	≥99%	￥10000.00 ￥1990.00 S88327-100mg ￥1990.00 现货	3 3	-	-	-	-

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产品描述：

JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.

靶点：

mGluR2:17 nM (EC50);GluR

体外研究：

JNJ-42153605 is assessed for its selectivity for the mGlu2 receptor and is found to not have agonist or antagonist activity toward other mGlu receptor subtypes up to 30 μM. JNJ-42153605 shows high permeability with no indication for P-glycoprotein efflux

体内研究：

JNJ-42153605 shows a central in vivo efficacy by inhibition of REM sleep state at a dose of 3 mg/kg po in the rat sleep-wake EEG paradigm, a phenomenon shown to be mGlu2 mediated. In mice, JNJ-42153605 shows reversed PCP-induced hyperlocomotion with an ED50 of 5.4 mg/kg sc, indicative of antipsychotic activity. JNJ-42153605 shows a rapid rate of absorption from the gastrointestinal tract, reaching the maximal concentration after 0.5 h. Clearance in vivo is moderate to high in both rat and dog (35 and 29 mL/min/kg, respectively). Elimination halflives are on the shorter side across the species, being 2.7 h in rat and 0.8-1.1 h in dog

参考文献：

1. Cid JM, et al. Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor. J Med Chem. 2012 Oct 25;55(20):8770-89.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.497 ml	12.486 ml	24.973 ml
5 mM	0.499 ml	2.497 ml	4.995 ml
10 mM	0.25 ml	1.249 ml	2.497 ml
50 mM	0.05 ml	0.25 ml	0.499 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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JNJ-42153605

3-(cyclopropylMethyl)-7-(4-phenylpiperidin-1-yl)-8-(trifluoroMethyl)-[1,2,4]triazolo[4,3-a]pyridine

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)