製品番号: HY-30234

Clemizole

Name: Clemizole
Brand: MedChemExpress
SKU: HY-30234
Price: 40.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Clemizole is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC₅₀ value of 1.05-1.34 μM against mouse TRPC5. Clemizole 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 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.

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純度 : 98.42%
CAS 番号: 442-52-4
分子式: C₁₉H₂₀ClN₃
分子量:325.84

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Clemizole 構造式

CAS 番号: 442-52-4

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Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

TRPC5

1.05-1.34 μM (IC₅₀)

TRP Channel アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>20 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	>20 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	>20 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	>20 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	11.3 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	26.5 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	6.4 μM Compound: 18	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	[PMID: 30943030]
HEK293	IC₅₀	9.1 μM Compound: 18	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	[PMID: 30943030]
Huh-7	CC₅₀	39.4 μM Compound: Clemizole	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	[PMID: 24561671]
Huh-7	EC₅₀	8 μM Compound: Clemizole	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	[PMID: 24561671]

体外実験

Viral InfectionOthersApoptosis

Viral Infection

Clemizole sulfate exhibits strong, synergistic anti-HCV activity in Huh 7.5 cells when combined with Boceprevir (HY-10237), with a synergy volume of 230 μM²%, and does not induce cellular toxicity at tested concentrations^[9].

Others

Clemizole sulfate (as Clemizole Hydrochloride) (1-10 μM; 24 h) significantly increases the viability of XP-C patient-derived fibroblasts exposed to UVB irradiation, with a dose-dependent protective effect that enhances photo-resistance compared to DMSO-treated cells^[11].
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].

Apoptosis

Clemizole sulfate (as Clemizole Hydrochloride) (10 μM; 24 h) does not reduce apoptosis or necrosis to mediate its protective effect 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.

Cell Viability Assay^[11]

Cell Line:

Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
Concentration:

10 μM (24 h pre-irradiation treatment); 10 μM (24 h post-irradiation treatment); 1-10 μM (both pre- and post-irradiation treatments)
Incubation Time:

24 h (pre-irradiation treatment); 24 h (post-irradiation treatment)
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.

Cell Viability Assay^[11]

Cell Line:

Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
Concentration:

0.1-10 μM (pre-irradiation only; post-irradiation only; combined pre- and post-irradiation treatments)
Incubation Time:

24 h post-UV
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.

Cell Proliferation Assay^[11]

Cell Line:

Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
Concentration:

10 μM (both pre- and post-irradiation treatments)
Incubation Time:

2 h post-UV; 4 h post-UV
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.

Apoptosis Analysis^[11]

Cell Line:

Xeroderma Pigmentosum C (XP-C) patient-derived immortalized fibroblasts (GM15983)
Concentration:

10 μM (both pre- and post-irradiation treatments)
Incubation Time:

24 h post-UV incubation
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.

体内実験

Oxidative StressInnate ImmunityCytokines & ChemokinesOthers

Oxidative Stress

Innate Immunity

Cytokines & Chemokines

Clemizole (10-30 mg/kg; i.p.; single dose) sulfate confers dose-dependent multifaceted neuroprotection in Sprague-Dawley rats with traumatic brain injury, with the 30 mg/kg dose producing the most pronounced improvements in neurological, sensorimotor, cognitive, and affective function, while restoring redox homeostasis, reducing neuronal damage, suppressing neuroinflammation, and preserving BBB integrity^[8].

Others

Clemizole (100-400 μM; p.o.; 30-min exposure; 90-min exposure) sulfate suppresses seizure-associated locomotion in scn1Lab mutant zebrafish larvae at doses of 100 μM (90-min exposure), 300 μM, and 400 μM (30-min exposure), with toxicity observed at higher concentrations during prolonged exposure^[10].
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.

Animal Model:

Sprague-Dawley Rat (6-8 weeks old)^[8]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

i.p.; single dose
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.

Animal Model:

TL strain (5 days post fertilization, undifferentiated sex)^[10]
Dosage:

100 μM (90-min exposure); 300 μM (30-min exposure); 400 μM (30-min exposure)
Administration:

p.o.; 30-min exposure; 90-min exposure
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.

Animal Model:

TL strain (5 days post fertilization, undifferentiated sex)^[10]
Dosage:

250 μM
Administration:

p.o.; single exposure
Result:

Significantly reduced mean swim velocity in scn1Laa mutant larvae, suppressing seizure behaviour similarly to known antiepileptic agents stiripentol and diazepam.

Related Protocols :

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

化学情報

CAS 番号 442-52-4
性状 Powder
分子量 325.84
分子式 C₁₉H₂₀ClN₃
Color White to off-white
SMILES

ClC1=CC=C(C=C1)CN2C(CN3CCCC3)=NC4=CC=CC=C24
輸送条件

Room temperature in continental US; may vary elsewhere.

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

bioRxiv

Cellular N-myristoyl transferases Are Required for Mammarenavirus Multiplication. [Abstract]

2024 Aug 1:2024.08.01.606235. PMID: 39211253

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0690 mL

15.3450 mL

30.6899 mL

5 mM

0.6138 mL

3.0690 mL

6.1380 mL

10 mM

0.3069 mL

1.5345 mL

3.0690 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Clemizole

1 Cited Publications

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Clemizole

MedChemExpress（MCE）の使用を引用している文献 Clemizole

TRP Channel アイソフォーム固有の製品をすべて表示

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