| 产品描述: | Clemizole is an H1 histamine receptor antagonist, can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication. |
| 靶点: |
HCV Protease;Histamine Receptor;HCVProtease; HistamineReceptor |
| 体内研究: |
Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours) which is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice |
| 细胞实验: |
Clemizole hydrochloride is dissolved in DMSO and stored, and then diluted with appropriate media before use. Huh7.5 cells are maintained in DMEM supplemented with 1% L-glutamine, 1% penicillin, 1% streptomycin, 1× nonessential amino acids and 10% FBS. Cell lines are passaged twice weekly after treatment with 0.05% trypsin-0.02% EDTA and seeding at a dilution of 1:5. Subconfluent Huh7.5 cells are trypsinized and collected by centrifugation at 700 g for 5 min. The cells are then washed three times in ice-cold RNase-free PBS and resuspended at 1.5×107 cells/mL in PBS. Wild-type or mutant FL-J6/JFH-5′C19Rluc2AUbi RNA for electroporation is generated by transcription of XbaI linearized DNA templates using the T7 MEGAscript kit, followed by purification (RNA transcription and fluorescent labeling). We mixed 5 μg of RNA with 400 μL of washed Huh7.5 cells in a 2-mm-gap cuvette (BTX) and immediately pulsed (0.82 kV, five 99 μs pulses) with a BTX-830 electroporator. After a 10 min recovery at 25°C, pulsed cells are dil |
| 参考文献: |
1. Richter JM, et al. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol Pharmacol. 2014 Nov;86(5):514-21. 2. Nishimura T, et al. Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction. J Pharmacol Exp Ther. 2013 Feb;344(2):388-96. 3. Einav S, et al. Discovery of a hepatitis C target and its pharmacological inhibitors by microfluidic affinity analysis. Nat Biotechnol. 2008 Sep;26(9):1019-27. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.069 ml |
15.345 ml |
30.69 ml |
| 5 mM |
0.614 ml |
3.069 ml |
6.138 ml |
| 10 mM |
0.307 ml |
1.534 ml |
3.069 ml |
| 50 mM |
0.061 ml |
0.307 ml |
0.614 ml |
|
| 注意: |
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