1. Anti-infection Autophagy
  2. Fungal Bacterial Autophagy Antibiotic
  3. Clotrimazole

Clotrimazole  (Synonyms: 克霉唑)

目录号: HY-10882 纯度: 99.91%
COA 产品使用指南

Clotrimazole是咪唑衍生物,有抗真菌活性,是P450抑制剂。Clotrimazole 还具有抗菌活性。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Clotrimazole Chemical Structure

Clotrimazole Chemical Structure

CAS No. : 23593-75-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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500 mg ¥500
In-stock
1 g ¥744
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5 g   询价  
10 g   询价  

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Customer Review

Other Forms of Clotrimazole:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.

IC50 & Target

Antifungal; CYP

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
5.1 μM
Compound: 1, CLT
Antiproliferative activity against human A549 cells by SRB assay
Antiproliferative activity against human A549 cells by SRB assay
[PMID: 19027297]
COS-7 IC50
0.07 μM
Compound: Clotrimazole
Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay
Inhibition of human cloned IK1 expressed in african green monkey COS7 cells by whole cell patch clamp assay
[PMID: 19282171]
CV-1 IC50
0.69 μM
Compound: 2
Inverse agonist activity at human CAR-LBD transfected in CV-1 cells after 24 hrs by luciferase reporter gene assay
Inverse agonist activity at human CAR-LBD transfected in CV-1 cells after 24 hrs by luciferase reporter gene assay
[PMID: 26717202]
HaCaT EC50
15 μM
Compound: Clotrimazole
Inhibition of human HaCaT cell proliferation after 48 hrs
Inhibition of human HaCaT cell proliferation after 48 hrs
[PMID: 19282171]
HEK293 IC50
0.59 μM
Compound: Clotrimazole
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
11.97 μM
Compound: Clotrimazole
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
[PMID: 28230985]
HEK-293T IC50
5.9 μM
Compound: Clotrimazole
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HEK-293T IC50
51.6 μM
Compound: Clotrimazole
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
[PMID: 23122865]
HEK-293T CC50
7 μg/mL
Compound: Clotrimazole
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 27720324]
HeLa IC50
1.4 μM
Compound: Clotrimazole
Inhibition of p97 in human HeLa cells assessed as reduction in p97-dependent UbG76V-GFP degradation incubated for 1 hr by luciferase reporter gene assay
Inhibition of p97 in human HeLa cells assessed as reduction in p97-dependent UbG76V-GFP degradation incubated for 1 hr by luciferase reporter gene assay
[PMID: 31550150]
HEp-2 CC50
18 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 24 hrs by trypan blue exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 24 hrs by trypan blue exclusion assay
[PMID: 27100030]
HEp-2 CC50
38 μg/mL
Compound: C
Cytotoxicity against human Hep2 cells assessed as reduction of cell viability after 24 hrs by trypan blue exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction of cell viability after 24 hrs by trypan blue exclusion assay
[PMID: 23702472]
HEp-2 CC50
38 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as cell survival after 24 hrs by trypan blue exclusion method
Cytotoxicity against human Hep2 cells assessed as cell survival after 24 hrs by trypan blue exclusion method
[PMID: 26562544]
HEp-2 CC50
38.8 μg/mL
Compound: Clotrimazole
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue dye exclusion assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability incubated for 24 hrs by trypan blue dye exclusion assay
[PMID: 28963991]
HEp-2 EC50
40 μg/mL
Compound: C
Cytotoxicity against human Hep2 cells assessed as cell survival fraction after 24 hrs by trypan blue exclusion method
Cytotoxicity against human Hep2 cells assessed as cell survival fraction after 24 hrs by trypan blue exclusion method
[PMID: 22560629]
HEp-2 EC50
48 μg/mL
Compound: C
Antiproliferative activity against human Hep2 cells assessed as cell survival fraction after 24 hrs by MTT assay
Antiproliferative activity against human Hep2 cells assessed as cell survival fraction after 24 hrs by MTT assay
[PMID: 22560629]
LLC-PK1 IC50
3.5 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
4.8 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
LLC-PK1 IC50
6.7 μM
Compound: Clotrimazole
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay
[PMID: 12699389]
MCF7 CC50
5 μg/mL
Compound: Clotrimazole
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
[PMID: 27720324]
NIH3T3 IC50
289.45 μg/mL
Compound: Clotrimazole
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 24 hrs by MTT assay
[PMID: 29274492]
Ventricular myocyte IC50
20 μM
Compound: Clotrimazole
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
体外研究
(In Vitro)

Clotrimazole (brand name Canesten or Lotrimin) is an antifungal medication commonly used in the treatment of fungal infections (of both humans and other animals) such as vaginal yeast infections, oral thrush, and ringworm. It is also used to treat athlete's foot and jock itch.It is commonly available as an over-the-counter substance in various dosage forms, such as a cream, and also (especially in the case of ear infection) as a combination medicine. It is also available as a troche or throat lozenge (prescription only). For ear infection, it is often applied in liquid form, as ear drops.? The antimycotic drug clotrimazole inhibits the function of the gastric H,K-ATPase in a manner similar to that observed for the Na,K-ATPase. Because of the high hydrophobicity of the compound, the interaction between clotrimazole and the ion pump occurs at the membrane domain in the apolar core of the membrane. The enzymatic activity was inhibited with a half-saturating concentration of 5.2 microM. Various partial reactions of the pump cycle were analyzed with the electrochromic styryl dye RH421 that has been widely used to study the transport mechanism of P-type ATPases.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

344.84

Formula

C22H17ClN2

CAS 号
性状

固体

颜色

White to off-white

中文名称

克霉唑;抗真菌1号;三苯甲咪唑

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 33.33 mg/mL (96.65 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8999 mL 14.4995 mL 28.9990 mL
5 mM 0.5800 mL 2.8999 mL 5.7998 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8999 mL 14.4995 mL 28.9990 mL 72.4974 mL
5 mM 0.5800 mL 2.8999 mL 5.7998 mL 14.4995 mL
10 mM 0.2900 mL 1.4499 mL 2.8999 mL 7.2497 mL
15 mM 0.1933 mL 0.9666 mL 1.9333 mL 4.8332 mL
20 mM 0.1450 mL 0.7250 mL 1.4499 mL 3.6249 mL
25 mM 0.1160 mL 0.5800 mL 1.1600 mL 2.8999 mL
30 mM 0.0967 mL 0.4833 mL 0.9666 mL 2.4166 mL
40 mM 0.0725 mL 0.3625 mL 0.7250 mL 1.8124 mL
50 mM 0.0580 mL 0.2900 mL 0.5800 mL 1.4499 mL
60 mM 0.0483 mL 0.2417 mL 0.4833 mL 1.2083 mL
80 mM 0.0362 mL 0.1812 mL 0.3625 mL 0.9062 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Clotrimazole
目录号:
HY-10882
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