Clemizole-d4
Based on 1 Customer Validation
Clemizole-d4 is the deuterated-labeled Clemizole (HY-30234). 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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.82%
- CAS 番号: 1251554-64-9
- 分子式: C19H16D4ClN3
- 分子量:329.86
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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
生物活性
製品説明
IC50 & Target
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TRPC5 1.05-1.34 μM (IC50) |
アプリケーション
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
化学情報
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CAS 番号 1251554-64-9
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非標識Cas 442-52-4
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性状 Solid
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分子量 329.86
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分子式 C19H16D4ClN3
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Color White to off-white
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SMILES
ClC1=C([2H])C([2H])=C(C([2H])=C1[2H])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
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (303.16 mM; ultrasonic and warming and heat to 80°C; 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)
純度とドキュメンテーション
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データシート (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
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]
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 | 3.0316 mL | 15.1579 mL | 30.3159 mL | 75.7897 mL |
| 5 mM | 0.6063 mL | 3.0316 mL | 6.0632 mL | 15.1579 mL | |
| 10 mM | 0.3032 mL | 1.5158 mL | 3.0316 mL | 7.5790 mL | |
| 15 mM | 0.2021 mL | 1.0105 mL | 2.0211 mL | 5.0526 mL | |
| 20 mM | 0.1516 mL | 0.7579 mL | 1.5158 mL | 3.7895 mL | |
| 25 mM | 0.1213 mL | 0.6063 mL | 1.2126 mL | 3.0316 mL | |
| 30 mM | 0.1011 mL | 0.5053 mL | 1.0105 mL | 2.5263 mL | |
| 40 mM | 0.0758 mL | 0.3789 mL | 0.7579 mL | 1.8947 mL | |
| 50 mM | 0.0606 mL | 0.3032 mL | 0.6063 mL | 1.5158 mL | |
| 60 mM | 0.0505 mL | 0.2526 mL | 0.5053 mL | 1.2632 mL | |
| 80 mM | 0.0379 mL | 0.1895 mL | 0.3789 mL | 0.9474 mL | |
| 100 mM | 0.0303 mL | 0.1516 mL | 0.3032 mL | 0.7579 mL |