Clotrimazole
(Synonyms: 克霉唑) 目录号 : GC16804
An imidazole antifungal
Cas No.:23593-75-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
MCF10A, MCF-7 and MDA-MB-231 human breast cancer cell lines |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
50 μM; 24 h |
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Applications |
In MCF10A, MCF-7 and MDA-MB-231 cells, Clotrimazole inhibited migration of MCF-7 and MDA-MB-231 cells by 32±5% and 59±6%, respectively, but had no effect on MCF10A cells. Clotrimazole inhibited mobility of MDA-MB-231 cells and MCF-7 cells. Also, clotrimazole reduced the viability of breast cancer cells. |
| Animal experiment [2]: | |
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Animal models |
CAL27 xenograft mice model |
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Dosage form |
150 mg/kg/body; 6 times a week for two weeks; intraperitoneally (i.p.) |
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Application |
In CAL27 xenograft mice model, clotrimazole significantly decreased the tumor volume of CAL27 cell xenograft in nude mice by 57.9%. Compared with control mice, the mean weights of the excised tumors were approximately 53.6% lower in clotrimazole-treated mice. Clotrimazole increased the number of apoptotic tumor cells. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Furtado CM1, Marcondes MC, Sola-Penna M, et al. Clotrimazole preferentially inhibits human breast cancer cell proliferation, viability and glycolysis. PLoS One. 2012;7(2):e30462. [2]. Wang J1, Jia L1, Kuang Z1, et al. The in vitro and in vivo antitumor effects of clotrimazole on oral squamous cell carcinoma. PLoS One. 2014 Jun 3;9(6):e98885. |
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Clotrimazole, bis-phenyl-(2-chlorophenyl)-1-imidazolyl methane, is a uniquely antifungal compound. In vitro, its spectrum includes dematiaceous, dermatophytes, dimorphic fungi and yeasts species. Its inhibitory concentrations in vitro were ≤ 4μg/mL for most susceptible fungi and ≤1 μg/mL for many species, particularly Trichophyton and Candida. Concentrations >20 μg/mL were fungicidal only [1]. It is also a specific Ca2+ activated K+ channel (Gardos channel) inhibitor [2]. Its IC50 to whole-cell currents in epithelial cells is 9 μmol/l [3].
Gardos channel contributes to pathologic water loss from erythrocytes and results in abnormal hemoglobin and promotes sickling in vitro. To avoid K+ and water loss via this channel was suggested as a potential therapy in vivo [2].
At concentrations ≤0.39 μg/mL, clotrimazole inhibited most isolates of C. neoformans, H. capsulatum and C. immitis. At concentrations < 0.78 μg/mL, clotrimazole did not inhibit one of C. neoformans. At 0.78 μg/mL, clotrimazole was fungicidal for all isolates, except a less susceptible isolate of H. capsulatum [1].
Subjects who had sickle cell anemia were treated with oral clotrimazole (10mg clotrimazole/kg/d for one week, and then daily dose was escalated by 10mg/kg each week). At a dosage of 20mg clotrimazole/kg/d, it was found that the Gardos channel was inhibited, cell K+ content was increased, erythrocyte dehydration was reduced, and hemoglobin levels was somewhat increased in all subjects. There are only three types of adverse effects, i.e. mild/moderate dysuria in all subjects and a reversible increase in plasma aspartic transaminase and alanine transaminase levels in two subjects treated with 30mg clotrimazole/kg/d [2].
References:
[1]. Smith Shadomy. In Vitro Antifungal Activity of Clotrimazole (Bay b 5097), Infection & Immunity. 1971, 4(2): 143-148.
[2]. Carlo Brugnara, Beatrice Gee, Carrie C. Armsby, et al. Therapy with Oral Clotrimazole Induces Inhibition of the Gardos Channel and Reduction of Erythrocyte Dehydration in Patients with Sickle Cell Disease. J. Clin. Invest., 1996, 97(5): 1227-1234.
[3]. Markus Bleich and Richard Warth. The very small-conductance K+ channel KVLQT1 and epithelial function. Pflügers Arch - Eur J Physiol, 2000, 440:202-206.
| Cas No. | 23593-75-1 | SDF | |
| 别名 | 克霉唑 | ||
| 化学名 | 1-[(2-chlorophenyl)-diphenylmethyl]imidazole | ||
| Canonical SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4 | ||
| 分子式 | C22H17ClN2 | 分子量 | 344.84 |
| 溶解度 | DMSO : 50 mg/mL; Ethanol : 15 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8999 mL | 14.4995 mL | 28.999 mL |
| 5 mM | 0.58 mL | 2.8999 mL | 5.7998 mL |
| 10 mM | 0.29 mL | 1.4499 mL | 2.8999 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。