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• 产品描述： Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM

• 靶点： mGlu5 Receptor:1.1 nM (Kd);GluR

• 体外研究：
  [3H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd of 1.1 nM. In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation with an IC50 of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues

• 体内研究：
  Basimglurant (RG7090) is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg)

• 参考文献：
  1. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. 2. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. J Med Chem. 2015 Feb 12;58(3):1358-71.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.07 ml	15.348 ml	30.697 ml
  5 mM	0.614 ml	3.07 ml	6.139 ml
  10 mM	0.307 ml	1.535 ml	3.07 ml
  50 mM	0.061 ml	0.307 ml	0.614 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 *