| 中文名称: | CTEP | ||||
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| 英文名称: | CTEP | ||||
| 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;CTEP (RO4956371) 国华试剂 RO 4956371; mGluR5 inhibitor;2-Chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine, RO4956371, 2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine | ||||
| CAS No: | 871362-31-1 | 分子式: | C19H13ClF3N3O | 分子量: | 391.77 |
| CAS No: | 871362-31-1 | ||||
| 分子式: | C19H13ClF3N3O | ||||
| 分子量: | 391.77 | ||||
基本信息
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产品编号： |
C11515 |
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产品名称： |
CTEP |
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CAS: |
871362-31-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃(密封储存) |
6个月 |
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分子量： |
391.77 |
-20℃(密封储存) |
1个月 |
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化学名： |
2-Chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine,RO4956371,2-Chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]-1H-imidazol-4-yl]ethynyl]pyridine |
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Solubility (25°C)： |
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体外:
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DMSO |
78mg/mL (199.09mM) |
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Ethanol |
10mg/mL (25.52mM) |
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Water |
Insoluble |
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体内(现配现用): |
2% DMSO+40% PEG 300+2% Tween 80+ddH2O |
9mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.5525mL |
12.7626mL |
25.5252mL |
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5mM |
0.5105mL |
2.5525mL |
5.1050mL |
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10mM |
0.2553mL |
1.2763mL |
2.5525mL |
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50mM |
0.0511mL |
0.2553mL |
0.5105mL |
生物活性
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产品描述 |
一种新颖的，长效的，可口服的 mGlu5 受体别构拮抗剂。 |
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靶点 |
mGlu5 |
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2.2nM |
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体外研究 |
CTEP (RO 4956371) inhibits quisqualate-induced Ca2+mobilization with an IC50 of 11.4nM and [3H]IP accumulation with an IC50 of 6.4nM in HEK293 cells stably expressing human mGlu5.CTEP (RO 4956371) inhibits the constitutive activity of human mGlu5 by approximately 50% with an IC50 of 40.1nM in HEK293 cells stably expressing human mGlu5. |
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体内研究 |
CTEP (RO 4956371) is significantly active at doses of 0.1mg/kg and 0.3mg/kg in treatment of anxiety in mouse.CTEP (RO 4956371) significantly increases drinking time at doses of 0.3mg/kg and 1.0mg/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 18h,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 8.7mg/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 2mg/kg p.o.every 48h for 2 months reaches a minimal CTEP (RO 4956371) brain exposure of 240ng/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 77.5ng/g measured in whole brain homogenate.CTEP (RO 4956371) (2mg/kg,p.o.bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice.CTEP (RO 4956371) (2mg/kg,p.o.) treatment corrects elevated hippocampal long-term depression,excessive protein synthesis,and audiogenic seizures in the Fmr1 knockout mouse. |
推荐实验方法(仅供参考)
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激酶实验： |
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For all filtration radioligand binding assays,membrane preparations expressing the target receptors or receptor combinations are resuspended in radioligand binding buffer (15mM Tris-HCl,120mM NaCl,5mM KCl,1.25 mM CaCl2,and 1.25mM MgCl2,pH 7.4),and the membrane suspension is mixed with the appropriate concentrations of radioligand and nonlabeled drugs in 96-well plates in a total volume of 200μL and incubated for 60 min at the appropriate temperature.At the end of the incubation,membranes are filtered onto Whatman Unifilter preincubated with 0.1% polyethyleneimine in ish buffer (50mM Tris-HCl,pH 7.4) with a Filtermate 196 harvester and washed three times with ice-cold ish buffer.Radioactivity captured on the filter is quantified on a Topcount microplate scintillation counter with quenching correction after the addition of 45μL of MicroScint 40 per well and shaking for 20 min.The concentration of membranes and incubation time is determined for each assay in pilot experiments. |
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动物实验: |
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Adult male Sprague-Dawley rats (body weight approximately 180-210g) and male NMRI mice (body weight approximately 25g) are supplied by Charles River.Rats are group-housed and mice are-single housed in separate holding rooms at controlled temperature (20-22℃) and 12-h light/dark cycle (lights on 6:00 AM).Animals are allowed ad libitum access to food and water,with the exception of those used in the Vogel conflict drinking test,where access to water is limited during the training sessions as described below.All formulations are prepared immediately before use in vehicle,consisting of 0.9% NaCl (w/v) and 0.3% Tween 80 (v/v) solution for oral administration of CTEP (RO 4956371),MPEP,MTEP,and fenobam;0.9% NaCl solution for MPEP and MTEP intravenously;and 30% N-methylpyrrolidone,42% hydroxypropyl-γ-cyclodextrin,and 28% water for fenobam intravenously.The volume of administration for oral dosing is 5mL/kg for rats,10mL/kg for mice,and 2.5mL/kg for intravenous applications and 10mL/kg for subcutaneous applications in mice. |
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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 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
