CTEP (RO4956371)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CTEP是一种新型、长效和可口服的代谢型谷氨酸受体5(mGlu5)抑制剂,IC50值为11.4 nM[1]。
CTEP是mGlu5的负变构调节剂,具有反向激动剂的活性。在体外结合实验中,CTEP与人、小鼠和大鼠的mGlu5结合,Kd值分别为1.7 nM、1.8 nM和1.5 nM。在表达mGlu5的HEK293细胞中,CTEP抑制quisqualate诱导的Ca2+动员和肌醇磷酸积累,IC50值分别为11.4 nM和6.4 nM。此外,在IP积累实验中,CTEP的IC50值40.1 nM,表明其反向激动剂活性。CTEP是mGlu5的高选择性抑制剂,在浓度高达10 μM时对mGlu1、mGlu2、mGlu3、mGlu4、mGlu6、mGlu7或mGlu8均没有显著的抑制活性[1]。
在体内沃格尔冲突饮水试验中,CTEP在0.3 mg/kg剂量时显著增加饮水次数。在成年C57BL / 6小鼠大脑中,CTEP在77.5 ng/g剂量时替换了mGlu5表达区域50%的mGlu5拮抗剂ABP688[1]。
参考文献:
[1] Lindemann L, Jaeschke G, Michalon A, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. Journal of Pharmacology and Experimental Therapeutics, 2011, 339(2): 474-486.
- 1. Choi WM, Kim HH, et al. "Glutamate Signaling in Hepatic Stellate Cells Drives Alcoholic Steatosis." Cell Metab. 2019 Aug 20. pii: S1550-4131(19)30430-9. PMID:31474565
- 2. Sun Y, Lipton JO, et al. "Direct current stimulation induces mGluR5-dependent neocortical plasticity." Ann Neurol. 2016 Aug;80(2):233-46. PMID:27315032
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 391.77 |
Cas No. | 871362-31-1 |
Formula | C19H13ClF3N3O |
Solubility | insoluble in EtOH; insoluble in H2O; ≥19.6 mg/mL in DMSO |
Chemical Name | 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine |
SDF | Download SDF |
Canonical SMILES | CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
激酶实验 [1]: | |
放射性配体结合分析 |
对于全部的过滤放射性配体结合实验来说,将表达靶受体或受体组合的膜制剂重悬浮于放射性配体结合缓冲液(15 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, 1.25 mM CaCl2和1.25 mM MgCl2, pH 7.4), 然后将重悬的膜与合适浓度的放射性配体以及未标记的药物在96孔板中混合,总体积200μL,适当温度下孵育60分钟。孵育结束后,用Filtermate 196 harvester将膜过滤到用0.1%聚乙烯亚胺洗涤缓冲液(50 mM Tris-HCl, pH 7.4)预孵育的Whatman Unifilter上,用冰冷的洗涤缓冲液洗三次。每孔加入45μL MicroScint 40然后摇晃20分钟之后,利用猝灭校正过的Topcount微闪烁计数器对在过滤器上捕获的放射性进行定量。膜的浓度和处理时间由每次的预实验决定。 |
动物实验: | |
动物模型 |
成年雄性C57BL/6小鼠模型;成年雄性Sprague-Dawley大鼠模型;Fmr1敲除小鼠模型 |
剂量 |
0.01-3.0mg / kg,口服灌胃,18小时;或2mg / kg,每48小时口服,持续2周 |
应用 |
CTEP(0.1和0.3 mg/kg)在小鼠应激诱导的高热过程和大鼠的Vogel冲突饮酒测试中具有剂量依赖性活性 [1]。 此外,在Fmr1基因敲除小鼠的海马中,CTEP纠正过度蛋白质合成,mGlu长期抑郁症和听源性癫痫发作 [2]。 |
注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
References: 1Lindemann, L., Jaeschke, G., Michalon, A., Vieira, E., Honer, M., Spooren, W., Porter, R., Hartung, T., Kolczewski, S., Buttelmann, B., Flament, C., Diener, C., Fischer, C., Gatti, S., Prinssen, E. P., Parrott, N., Hoffmann, G. and Wettstein, J. G. (2011) CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 339, 474-486 2Michalon, A., Sidorov, M., Ballard, T. M., Ozmen, L., Spooren, W., Wettstein, J. G., Jaeschke, G., Bear, M. F. and Lindemann, L. (2012) Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 74, 49-56 |
描述 | CTEP (RO4956371)是一种新型、长效和可口服的mGlu5受体变构拮抗剂,IC50值为2.2 nM。 | |||||
靶点 | mGlu5 receptor | |||||
IC50 | 2.2 nM |
质量控制和MSDS
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