Clemizole hydrochloride
Based on 1 publication(s) in Google Scholar
Clemizole (EPX-100) hydrochloride is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole hydrochloride blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole hydrochloride can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.99%
- CAS No.: 1163-36-6
- Formule: C19H21Cl2N3
- Masse moléculaire:362.30
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Clemizole hydrochloride
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Activité biologique
Description
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TRPC5 1.05-1.34 μM (IC50) |
5-HT2A Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Vero C1008 | CC50 |
>40 μM
Compound: Clemizole hydrochloride
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Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)
Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)
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10.1101/2020.04.03.023846 |
| Vero C1008 | EC50 |
23.94 μM
Compound: Clemizole hydrochloride
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Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days
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10.1101/2020.04.03.023846 |
In Vitro
Clemizole sulfate (as Clemizole Hydrochloride) (5 μM; 24 h) significantly promotes repair of UVB-induced 6-4PP DNA lesions in XP-C patient-derived fibroblasts[11].
Clemizole sulfate (as Clemizole Hydrochloride) (0.1-10 μM; 24 h) mediates enhanced UVB photo-resistance in XP-C patient-derived fibroblasts through both pre- and post-UVB irradiation treatment, with the combined regimen yielding the highest bioactivity[11].
Clemizole sulfate (as Clemizole Hydrochloride) (10 μM; 2-4 h) does not affect DNA replication or cell proliferation in XP-C patient-derived fibroblasts exposed to UVB irradiation[11].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
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Concentration:10 μM (24 h pre-irradiation treatment); 10 μM (24 h post-irradiation treatment); 1-10 μM (both pre- and post-irradiation treatments)
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Incubation Time:24 h (pre-irradiation treatment); 24 h (post-irradiation treatment)
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Result:Showed ≥25% photo-resistance and a robust Z score above 2.6 in primary screen.
Induced a significant 20 to 40% increase in XP-C cell viability depending on UVB dose and reagent concentration, with increased bioactivity at higher concentrations.
Significantly enhanced photo-resistance in XP-C cells across increasing UVB doses, with viability remaining higher than DMSO-treated controls at all tested UVB doses.
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Cell Line:Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
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Concentration:0.1-10 μM (pre-irradiation only; post-irradiation only; combined pre- and post-irradiation treatments)
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Incubation Time:24 h post-UV
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Result:Reached ~20% increased cell viability at 10 μM with pre-irradiation treatment alone.
Reached an average of ~50% increased viability at 10 μM with post-irradiation treatment alone.
Showed the highest bioactivity with combined pre- and post-irradiation treatment, with a significant increase compared to pre-treatment alone at both 5 μM and 10 μM, and no significant difference compared to post-treatment alone.
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Cell Line:Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
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Concentration:10 μM (both pre- and post-irradiation treatments)
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Incubation Time:2 h post-UV; 4 h post-UV
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Result:Showed no significant increase in EdU mean fluorescence intensity (MFI) compared to DMSO-treated cells at 2 h or 4 h post-UV.
Showed no significant difference in the percentage of EdU-positive cells from DMSO-treated cells at either time point, indicating no enhancement of DNA replication or cell proliferation.
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Cell Line:Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
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Concentration:10 μM (both pre- and post-irradiation treatments)
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Incubation Time:24 h post-UV incubation
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Result:Did not show a significant decrease in apoptotic (CellEvent-positive) or necrotic (PI-positive) cell populations compared to DMSO-treated cells.
Did not significantly increase the live cell population.
In Vivo
Clemizole (250 μM; p.o.; single exposure) sulfate significantly suppresses seizure-associated locomotion in scn1Laa mutant zebrafish larvae, a second Dravet syndrome model[10].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley Rat (6-8 weeks old)[8]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; single dose
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Result:Promoted neurological function recovery after TBI in a dose-dependent manner.
Improved sensorimotor dysfunction after TBI.
Reversed TBI-related anxiety-like behaviors.
Improved spatial learning and memory deficits after TBI without affecting motor function.
Alleviated TBI-induced oxidative stress and restored antioxidant defense capabilities.
Alleviated TBI-induced cortical cell damage.
Inhibited microglia and astrocyte activation, reduced pro-inflammatory cytokine levels, and restored tight junction protein expression, thus protecting the integrity of the blood-brain barrier.
Activated the PI3K-Akt pro-survival pathway, downregulated the Bax/Bcl-2 ratio, and inhibited the caspase cascade, thus exerting an anti-apoptotic effect.
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Animal Model:TL strain (5 days post fertilization, undifferentiated sex)[10]
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Dosage:100 μM (90-min exposure); 300 μM (30-min exposure); 400 μM (30-min exposure)
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Administration:p.o.; 30-min exposure; 90-min exposure
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Result:Suppressed seizure-related locomotion at 300 μM and 400 μM (30-min exposure) and at 100 μM (90-min exposure), reducing mean swim velocity by ≥40%.
Caused toxicity at 300 μM and 400 μM during prolonged 90-min exposure.
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Animal Model:TL strain (5 days post fertilization, undifferentiated sex)[10]
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Dosage:250 μM
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Administration:p.o.; single exposure
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Result:Significantly reduced mean swim velocity in scn1Laa mutant larvae, suppressing seizure behaviour similarly to known antiepileptic agents stiripentol and diazepam.
- Research Protocol for Infectious Diseases
- Nephrotoxicity Study
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- CCK-8/WST-8 Cell Proliferation Assay
- Research Protocol for Neurological Diseases
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 1163-36-6
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Appearance Solid
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Masse moléculaire 362.30
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Formule C19H21Cl2N3
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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.[H]Cl
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Synonyms
EPX-100
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (92.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (55.20 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (5.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.38 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (311 KB)
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SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
- Italian - IT (596 KB)
- Korean - KR (596 KB)
- Portuguese - PT (596 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Richter JM, et al. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Molecular pharmacology. 2014 Nov;86(5):514-21. [Content Brief]
[2]. Baraban SC, et al. Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment. Nature communications. 2013;4:2410. [Content Brief]
[3]. Jie LJ, et al. Clemizole hydrochloride blocks cardiac potassium currents stably expressed in HEK 293 cells. British journal of pharmacology. 2017 Feb;174(3):254-266. [Content Brief]
[4]. Einav S, et al. Discovery of a hepatitis C target and its pharmacological inhibitors by microfluidic affinity analysis. Nature biotechnology. 2008 Sep;26(9):1019-27. [Content Brief]
[5]. Yu H, et al. Clemizole inhibits CrtN-driven staphyloxanthin biosynthesis in Staphylococcus aureus to enhance host immune clearance. Communications biology. 2026 Feb 25;9(1):484. [Content Brief]
[6]. Kumaş-Kulualp M, et al. Clemizole hydrochloride, a potent TRPC5 calcium channel inhibitor, prevents cisplatin-induced nephrotoxicity in Spraque-Dawley rats. Journal of biochemical and molecular toxicology. 2023 Jul;37(7):e23372. [Content Brief]
[7]. Moog M, et al. Clemizole and trazodone are effective antiseizure treatments in a zebrafish model of STXBP1 disorder. Epilepsia open. 2022 Sep;7(3):504-511. [Content Brief]
[8]. Chauhan C, et al. Clemizole Mitigates Traumatic Brain Injury by Inhibiting Oxidative Stress, Neuroinflammation, and Apoptosis. ACS chemical neuroscience. 2026 May 06;17(9):1787-1801. [Content Brief]
[9]. Nishimura T, et al. Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction. The Journal of pharmacology and experimental therapeutics. 2013 Feb;344(2):388-96. [Content Brief]
[10]. Griffin A, et al. Clemizole and modulators of serotonin signalling suppress seizures in Dravet syndrome. Brain : a journal of neurology. 2017 Mar 01;140(3):669-683. [Content Brief]
[11]. Kobaisi F, et al. Isoconazole and Clemizole Hydrochloride Partially Reverse the Xeroderma Pigmentosum C Phenotype. International journal of molecular sciences. 2021 Jul 29;22(15):8156. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.7601 mL | 13.8007 mL | 27.6014 mL | 69.0036 mL |
| 5 mM | 0.5520 mL | 2.7601 mL | 5.5203 mL | 13.8007 mL | |
| 10 mM | 0.2760 mL | 1.3801 mL | 2.7601 mL | 6.9004 mL | |
| 15 mM | 0.1840 mL | 0.9200 mL | 1.8401 mL | 4.6002 mL | |
| 20 mM | 0.1380 mL | 0.6900 mL | 1.3801 mL | 3.4502 mL | |
| 25 mM | 0.1104 mL | 0.5520 mL | 1.1041 mL | 2.7601 mL | |
| 30 mM | 0.0920 mL | 0.4600 mL | 0.9200 mL | 2.3001 mL | |
| 40 mM | 0.0690 mL | 0.3450 mL | 0.6900 mL | 1.7251 mL | |
| 50 mM | 0.0552 mL | 0.2760 mL | 0.5520 mL | 1.3801 mL | |
| DMSO | 60 mM | 0.0460 mL | 0.2300 mL | 0.4600 mL | 1.1501 mL |
| 80 mM | 0.0345 mL | 0.1725 mL | 0.3450 mL | 0.8625 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Clemizole hydrochloride Related Classifications
HY-30234A Related Classifications
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Keywords
- Clemizole
- 1163-36-6
- EPX-100
- EPX100
- EPX 100
- TRP Channel
- Apoptosis
- 5-HT Receptor
- Transient receptor potential channels
- Serotonin Receptor
- 5-hydroxytryptamine Receptor
- XP-C patient-derived fibroblasts
- Huh 7.5 cells
- Sprague-Dawley rats
- S. aureus CrtN
- histamine H1
- human HCV NS4B
- blood-brain barrier
- mouse TRPC5
- TRPC5
- scn1Lab mutant zebrafish larvae
- Inhibitor
- inhibitor
- inhibit