货号	规格	价格	上海	北京	珠海	重庆	武汉
S81042-1mg买3赠1	99.30%	￥260.00 S81042-1mg ￥260.00 现货（买3赠1）	9 9	-	-	-	-
S81042-5mg买3赠1	99.30%	￥440.00 S81042-5mg ￥440.00 现货（买3赠1）	6 6	-	-	-	-
S81042-10mg买3赠1	99.30%	￥780.00 S81042-10mg ￥780.00 现货（买3赠1）	5 5	-	-	-	-
S81042-25mg促销	99.30%	￥1500.00 ￥1200.00 S81042-25mg ￥1200.00 现货	5 5	-	-	-	-
S81042-50mg促销	≥97%	￥2230.00 ￥1780.00 S81042-50mg ￥1780.00 2-3天	0 货期：2-3天	-	-	-	-
S81042-100mg促销	≥97%	￥3270.00 ￥2610.00 S81042-100mg ￥2610.00 2-3天	0 货期：2-3天	-	-	-	-

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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

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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CTEP (RO4956371)