Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CTEP (RO 4956371) 是一种新型、长效、可口服的 mGlu5 受体变构拮抗剂,IC50 为 2.2 nM,比其他 mGlu 受体选择性高 1000 倍以上。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 473 | 现货 | ||
2 mg | ¥ 625 | 现货 | ||
5 mg | ¥ 788 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,690 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,820 | 现货 | ||
500 mg | ¥ 11,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 871 | 现货 |
产品描述 | CTEP (RO 4956371) (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. |
靶点活性 | mGlu5:2.2 nM |
体外活性 | CTEP inhibits quisqualate-induced Ca2+ mobilization with an IC50 of 11.4 nM and [3H]IP accumulation with an IC50 of 6.4 nM in HEK293 cells stably expressing human mGlu5. 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. [1] |
体内活性 | CTEP is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP 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 (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 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 brain exposure of 240 ng/g. CTEP 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. [1] CTEP (2 mg/kg p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (2 mg/kg p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse. [2] |
激酶实验 | For all filtration radioligand binding assays, membrane preparations expressing the target receptors or receptor combinations are resuspended in radioligand binding buffer (15 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, 1.25 mM CaCl2, and 1.25 mM 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 200 μL 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 (50 mM 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 45 μL 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. |
别名 | mGluR5 inhibitor, RO 4956371 |
分子量 | 391.77 |
分子式 | C19H13ClF3N3O |
CAS No. | 871362-31-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 10 mg/mL (25.52 mM)
DMSO: 72 mg/mL (183.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.5525 mL | 12.7626 mL | 25.5252 mL | 63.813 mL |
5 mM | 0.5105 mL | 2.5525 mL | 5.105 mL | 12.7626 mL | |
10 mM | 0.2553 mL | 1.2763 mL | 2.5525 mL | 6.3813 mL | |
20 mM | 0.1276 mL | 0.6381 mL | 1.2763 mL | 3.1906 mL | |
DMSO | 50 mM | 0.0511 mL | 0.2553 mL | 0.5105 mL | 1.2763 mL |
100 mM | 0.0255 mL | 0.1276 mL | 0.2553 mL | 0.6381 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CTEP 871362-31-1 Neuroscience GluR Metabotropic glutamate receptors inhibit mGluR5 inhibitor mGluR RO 4956371 RO-4956371 Inhibitor RO4956371 inhibitor