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• 产品描述： ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities

• 靶点： mGluR5:0.17 μM (EC50);GluR

• 体内研究：
  ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex. ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats. ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice. ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats. ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice.

• 参考文献：
  1. Liu F, et al. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive 2. Schlumberger C, et, al. Effects of a positive allosteric modulator of mGluR5 ADX47273 on conditioned avoidance response and PCP-induced hyperlocomotion in the rat as models for schizophrenia. Pharmacol Biochem Behav. 2010 Mar;95(1):23-30. 3. Xu J, et al. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learn Mem. 2013 Jul 18;20(8):438-45.

• 溶解性： DMSO  :  ≥  31  mg/mL  (83.93  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.707 ml	13.537 ml	27.074 ml
  5 mM	0.541 ml	2.707 ml	5.415 ml
  10 mM	0.271 ml	1.354 ml	2.707 ml
  50 mM	0.054 ml	0.271 ml	0.541 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

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

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *