产品说明书

CTEP

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Chemical Structure| 871362-31-1 同义名 : RO 4956371;mGluR5 inhibitor
CAS号 : 871362-31-1
货号 : A170773
分子式 : C19H13ClF3N3O
纯度 : 98%+
分子量 : 391.774
MDL号 : MFCD22665726
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(268.01 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+40% PEG 300+2% Tween 80+water 9 mg/mL

生物活性
靶点

  • mGluR5

    mGlu5, IC50:2.2 nM
描述 CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM. CTEP binds mGlu5 with low nanomolar affinity and shows > 1000-fold selectivity over other mGlu receptors. In vivo, CTEP is active in the stress-induced hyperthermia procedure in mice and the Vogel conflict drinking test in rats with minimal effective doses of 0.1 and 0.3 mg/kg. In vitro, CTEP inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1 nM in HEK293 cells stably expressing human mGlu5[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.76mL

2.55mL

1.28mL

25.52mL

5.10mL

2.55mL
参考文献

[1]Michalon A, Sidorov M, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 2012 Apr 12;74(1):49-56.

[2]Lindemann L, Jaeschke G, 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.

[3]Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. doi: 10.1124/jpet.111.185660. Epub 2011 Aug 17. PMID: 21849627.