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• 产品描述： CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.

• 靶点： mGlu5 Receptor:2.2 nM (IC50);GluR

• 体内研究：
  CTEP (RO 4956371) is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP (RO 4956371) significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (RO 4956371) (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP (RO 4956371) formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP (RO 4956371) brain exposure of 240 ng/g. CTEP (RO 4956371) fully displaces [3H]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate. CTEP (RO 4956371) (2 mg/kg, p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (RO 4956371) (2 mg/kg, p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse

• 参考文献：
  1. Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. 2. Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 2012 Apr 12;74(1):49-56.

• 溶解性： DMSO  :  ≥  100  mg/mL  (255.25  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.553 ml	12.763 ml	25.525 ml
  5 mM	0.511 ml	2.553 ml	5.105 ml
  10 mM	0.255 ml	1.276 ml	2.553 ml
  50 mM	0.051 ml	0.255 ml	0.511 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 *