2. Anti-infection Autophagy Apoptosis MAPK/ERK Pathway Cytoskeleton Cell Cycle/DNA Damage
  3. Fungal Autophagy Apoptosis p38 MAPK Microtubule/Tubulin
  4. Sertaconazole nitrate

Sertaconazole nitrate  (Synonyms: 硝酸舍他康唑; FI7056)

目录号: HY-B0736A 纯度: 99.58%
COA 产品使用指南

摩尔计算器

Sertaconazole nitrate (FI7056) 是一种局部广谱的抗真菌剂，可通过激活 p38-COX-2-PGE 2 通路来发挥抗炎活性。Sertaconazole nitrate 也是一种微管蛋白抑制剂，具有抗癌细胞增殖活性，诱导细胞的凋亡和自噬，还能抑制细胞的迁移，具有较好的抗癌活性。

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Sertaconazole nitrate Chemical Structure

Sertaconazole nitrate Chemical Structure

CAS No. : 99592-39-9

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥500
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5 mg ￥281
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10 mg ￥450
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50 mg ￥750
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100 mg ￥1200
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500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Sertaconazole nitrate:

Sertaconazole nitrate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells[1][2][3][4].

体外研究
(In Vitro)

Sertaconazole nitrate (0.03-40 µg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 µg/mL[1].
Sertaconazole nitrate (1 µg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner[2].
Sertaconazole nitrate (1, 2 µg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation[2].
Sertaconazole nitrate (10, 20, 30, 40 µM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect[3].
Sertaconazole nitrate (20, 40 µM; 24 h) induces apoptosis through p53 pathway in HeLa cells[3].
Sertaconazole nitrate (20, 30 µM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner[3].
Sertaconazole nitrate (15, 30 µM; 24 h) induces autophagy in A549, H460 cells[4].

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

Sertaconazole nitrate 相关抗体:

Cell Viability Assay[1]

Cell Line: C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata
Concentration: 0.03-40 µg/mL
Incubation Time: 24 h
Result: Againsted 150 strains of yeasts (six Candida species) which included C. albicans, C. guilliermondii, C. krusei, C. parapsilosi, C. tropicalis, C. glabrata species with arithmetic mean MIC values of 1.02, 0.51, 0.38, 0.31, 1.67 and 0.78 µg/mL, respectively.

Western Blot Analysis[2]

Cell Line: HaCaT cells
Concentration: 1 µg/mL
Incubation Time: 5, 10, 30, 60 min
Result: Showed activity of activating p38 MAP kinase and Hsp27 in a time-dependent manner.

Western Blot Analysis[2]

Cell Line: HaCaT cells
Concentration: 1, 2 µg/mL
Incubation Time: 6 or 8 h
Result: Induced 50% expression of COX-2 and resulted in a twofold increased in PGE2 release.

Western Blot Analysis[2]

Cell Line: siRNA-transfected HaCaT cells (without p38 MAP kinase expression)
Concentration: 1 µg/mL
Incubation Time: 24 h
Result: Mediated induction of PGE2 was dependent on p38 activation.

Cell Proliferation Assay[3]

Cell Line: HeLa, HEK-293, MCF-7, A549 cells
Concentration: 0-100 µM
Incubation Time: 24 h
Result: Showed antiproliferation activity with IC50s of 38, 45.1, 41.5, and 40.8 μM for HeLa, HEK-293, A549, and MCF-7 cells, respectively.
Exhibited mitotic block activity and induced cell death at concentration above 30 μM, but no significant increased in the number of mitotic cells.
Depolymerized interphase and spindle microtubules inducing defect in chromosomal congression.

Apoptosis Analysis[3]

Cell Line: HeLa cells
Concentration: 10, 20, 40 µM
Incubation Time: 24 h
Result: Induced approximately 5%, 10%, and 21% cells apoptotic at concentrations of 10, 20 and 40 μM, respectively.

Western Blot Analysis[3]

Cell Line: A549 cells
Concentration: 20, 40 µM
Incubation Time: 24 h
Result: Induced apoptosis through p53 pathway that the expression of p53 from 30% to 50% and 95% and p21 from 11 to 39% and 40% respectively.
Resulted in Noxa and Puma, two direct transcriptional targets of p53 to be overexpressed.

Cell Migration Assay [3]

Cell Line: HeLa cells
Concentration: 20, 30 µM
Incubation Time: 24, 48, and 72 h
Result: Inhibited the migration of HeLa cells at concentrations lesser than its IC50, which in a concentration-dependent manner.

Cell Autophagy Assay[4]

Cell Line: A549, H460 cells
Concentration: 15, 30 µM
Incubation Time: 24 h
Result: Increased endogenous LC3 puncta and LC3 intensity, which indicated induction of autophagy in A549 and H460 cells.
体内研究
(In Vivo)

Sertaconazole nitrate (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice[2].

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

Animal Model: CD-1 mice (TPA-induced ear edema model)[2].
Dosage: 1% (w/v)
Administration: Apply to the left ear, once.
Result: Exhibited a significant reduction of inflammation in mice by mediating PGE2 release.
Clinical Trial
分子量

500.78

Formula

C20H16Cl3N3O4S
CAS 号
性状

固体

颜色

White to off-white

中文名称

硝酸舍他康唑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (199.69 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9969 mL 9.9844 mL 19.9688 mL
5 mM 0.3994 mL 1.9969 mL 3.9938 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

  • 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 (4.99 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。

    以 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 (4.99 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。

    以 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

只
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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Sertaconazole nitrate 相关分类

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9969 mL 9.9844 mL 19.9688 mL 49.9221 mL
5 mM 0.3994 mL 1.9969 mL 3.9938 mL 9.9844 mL
10 mM 0.1997 mL 0.9984 mL 1.9969 mL 4.9922 mL
15 mM 0.1331 mL 0.6656 mL 1.3313 mL 3.3281 mL
20 mM 0.0998 mL 0.4992 mL 0.9984 mL 2.4961 mL
25 mM 0.0799 mL 0.3994 mL 0.7988 mL 1.9969 mL
30 mM 0.0666 mL 0.3328 mL 0.6656 mL 1.6641 mL
40 mM 0.0499 mL 0.2496 mL 0.4992 mL 1.2481 mL
50 mM 0.0399 mL 0.1997 mL 0.3994 mL 0.9984 mL
60 mM 0.0333 mL 0.1664 mL 0.3328 mL 0.8320 mL
80 mM 0.0250 mL 0.1248 mL 0.2496 mL 0.6240 mL
100 mM 0.0200 mL 0.0998 mL 0.1997 mL 0.4992 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.

Keywords:

Sertaconazole99592-39-9FI7056硝酸舍他康唑FI 7056FI-7056FungalAutophagyApoptosisp38 MAPKMicrotubule/TubulinCandidaPGE2COX-2HaCaTHeLaHEK-293MCF-7A549Inhibitorinhibitorinhibit

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