CTEP (RO4956371)|871362-31-1|(RO 4956371; mGluR5 inhibitor)-陌孚医药/Medlife

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CTEP (RO4956371) (Synonyms: RO 4956371; mGluR5 inhibitor)

目录号: PC10739 纯度: ≥98%

CAS No. :871362-31-1

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中文名称	CTEP (RO4956371)
中文别名	2-氯-4-[[2,5-二甲基-1-[4-(三氟甲氧基)苯基]-1H-咪唑-4-基]乙炔基]吡啶;mGlu5受体变构拮抗剂CTEP
英文名称	CTEP (RO4956371)
英文别名	2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine;CTEP;AGN-PC-00DCC8;CS-0974;AM808005;HY-15445;KB-76209;2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine;CTEP (RO4956371);mGluR5 inhibitor;2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine;RO4956371;[3H]CTEP;C19H13ClF3N3O;GTPL6409;GTPL6408;HMS3651N19;BCP06140;AOB87758;BDBM50071375;s2861;2340AH;compound 3 [PMID: 25565255];AM80
Cas No.	871362-31-1
分子式	C₁₉H₁₃ClF₃N₃O
分子量	391.77
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

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.

性状

Solid

IC50 & Target[1][2]

mGlu5 Receptor

2.2 nM (IC₅₀)

体外研究(In Vitro)

CTEP (RO 4956371) inhibits quisqualate-induced Ca mobilization with an IC₅₀ of 11.4 nM and [H]IP accumulation with an IC₅₀ of 6.4 nM in HEK293 cells stably expressing human mGlu5. CTEP (RO 4956371) inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC₅₀ of 40.1 nM in HEK293 cells stably expressing human mGlu5.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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 [H]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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

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. [Information]

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

溶解度数据

体外研究:

DMSO : ≥ 100 mg/mL (255.25 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5525 mL	12.7626 mL	25.5252 mL
5 mM	0.5105 mL	2.5525 mL	5.1050 mL
10 mM	0.2553 mL	1.2763 mL	2.5525 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.38 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.38 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.38 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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