Clemizole
Based on 1 publication(s) in Google Scholar
Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole is an inhibitor of TRPC5 channel. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
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- 純度: 98.42%
- CAS 番号: 442-52-4
- 分子式: C19H20ClN3
- 分子量:325.84
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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MedChemExpress（MCE）の使用を引用している文献 Clemizole
MoreHistamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>20 μM
Compound: 18
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Inhibition of CFP-tagged rat TRPV1 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
Inhibition of CFP-tagged rat TRPV1 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
>20 μM
Compound: 18
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Inhibition of YFP-tagged mouse TRPV4 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged mouse TRPV4 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
>20 μM
Compound: 18
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Inhibition of YFP-tagged rat TRPV2 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged rat TRPV2 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
>20 μM
Compound: 18
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Inhibition of YFP-tagged rat TRPV3 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged rat TRPV3 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
11.3 μM
Compound: 18
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Inhibition of YFP-tagged human TRPC6 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged human TRPC6 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
26.5 μM
Compound: 18
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Inhibition of YFP-tagged mouse TRPC7 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged mouse TRPC7 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
6.4 μM
Compound: 18
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Inhibition of YFP-tagged mouse TRPC4 beta expressed in thapsigargin treated HEK293 cells co-expressing M3 receptor assessed as reduction in carbachol-induced calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged mouse TRPC4 beta expressed in thapsigargin treated HEK293 cells co-expressing M3 receptor assessed as reduction in carbachol-induced calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
9.1 μM
Compound: 18
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Inhibition of YFP-tagged human TRPC3 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
Inhibition of YFP-tagged human TRPC3 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay
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[PMID: 30943030] |
| Huh-7 | CC50 |
39.4 μM
Compound: Clemizole
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Cytotoxicity against human Huh7.5 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human Huh7.5 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 24561671] |
| Huh-7 | EC50 |
8 μM
Compound: Clemizole
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Antiviral activity against Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells assessed as inhibition of viral RNA replication after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus JFH-1 J6 genotype 2a infected in human Huh7.5 cells assessed as inhibition of viral RNA replication after 72 hrs by luciferase reporter gene assay
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[PMID: 24561671] |
Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B’s RNA binding, with little toxicity for the host cell. The EC50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC50 of the wild-type RNA)[1]. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50=1.0-1.3 µM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC50=6.4 µM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC50=9.1 µM) and TRPC6 (IC50=11.3 µM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 µM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC50 of 1.1±0.04 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 442-52-4
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性状 Powder
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分子量 325.84
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分子式 C19H20ClN3
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Color White to off-white
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SMILES
ClC1=CC=C(C=C1)CN2C(CN3CCCC3)=NC4=CC=CC=C24
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2024 Aug 1:2024.08.01.606235. PMID: 39211253
溶剤 & 溶解度
DMSO : 50 mg/mL (153.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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 700g 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 diluted into 10 mL of prewarmed growth medium. Cells from several electroporations are pooled to a common stock and seeded in 6-well plates (5×105 cells per well). After 24 h, medium is replaced and cells are grown in the presence of serial dilutions of the various inhibitory compounds (e.g., Clemizole hydrochloride) identified in the screen. Seventeen commercially available compounds, out of the 18 identified, are analyzed. Untreated cells are used as a negative control for water-soluble compounds. For compounds (e.g., Clemizole hydrochloride) solubilized in DMSO, untreated cells are grown in the presence of corresponding concentrations of the solvent as a negative control. Medium is changed daily. After 72 h of treatment cells are subjected to an Alamar Blue-based viability assay and luciferase assay. After 72 h of treatment cells are incubated for 3 h at 37°C in the presence of 10% Alamar Blue reagent. Plates are then scanned and fluorescence is detected by using FLEXstation II 384. Depending on the inhibitory compound’s solvent (e.g., Clemizole hydrochloride), water or DMSO, signal is normalized relatively to untreated samples or samples grown in the presence of DMSO, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Eight control NOG mice and eight humanized TK-NOG mice are administered 25 mg/kg by mouth Clemizole, and blood samples are collected 30 minutes after administration. The C57BL/6J mice (3 per time point) are given 25 mg/kg by mouth clemizole, and blood samples are collected for analysis at 15 and 30 minutes and 1, 2, 4, and 6 hours after administration. For the DDI studies, eight humanized TK-NOG mice are given Clemizole (25 mg/kg by mouth) with or without Ritonavir (20 mg/kg by mouth), and blood samples are collected 30 minutes after administration. Six of these mice are also treated with Debrisoquine (10 mg/kg by mouth) in the presence or absence of Ritonavir (20 mg/kg by mouth), and plasma samples are obtained 2 hours later for analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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データシート (284 KB)
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- English - EN (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. 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 [Content Brief]
[2]. 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 [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0690 mL | 15.3450 mL | 30.6899 mL | 76.7248 mL |
| 5 mM | 0.6138 mL | 3.0690 mL | 6.1380 mL | 15.3450 mL | |
| 10 mM | 0.3069 mL | 1.5345 mL | 3.0690 mL | 7.6725 mL | |
| 15 mM | 0.2046 mL | 1.0230 mL | 2.0460 mL | 5.1150 mL | |
| 20 mM | 0.1534 mL | 0.7672 mL | 1.5345 mL | 3.8362 mL | |
| 25 mM | 0.1228 mL | 0.6138 mL | 1.2276 mL | 3.0690 mL | |
| 30 mM | 0.1023 mL | 0.5115 mL | 1.0230 mL | 2.5575 mL | |
| 40 mM | 0.0767 mL | 0.3836 mL | 0.7672 mL | 1.9181 mL | |
| 50 mM | 0.0614 mL | 0.3069 mL | 0.6138 mL | 1.5345 mL | |
| 60 mM | 0.0511 mL | 0.2557 mL | 0.5115 mL | 1.2787 mL | |
| 80 mM | 0.0384 mL | 0.1918 mL | 0.3836 mL | 0.9591 mL | |
| 100 mM | 0.0307 mL | 0.1534 mL | 0.3069 mL | 0.7672 mL |
Clemizole 関連分類
HY-30234 関連分類
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