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Sertaconazole nitrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sertaconazole nitrate图片
CAS NO:99592-39-9
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
硝酸舍他康唑
FI7056
产品介绍
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。
生物活性

Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of ap38-COX-2-PGE2pathway. Sertaconazole nitrate is also amicrotubuleinhibitor, shows antiproliferative effect, inducesapoptosisandautophagy, 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 sixCandidaspecies 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].

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 (sixCandidaspecies) which includedC. albicans,C. guilliermondii,C. krusei,C. parapsilosi,C. tropicalis,C. glabrataspecies 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].

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

性状

Solid

Formula

C20H16Cl3N3O4S

CAS 号

99592-39-9

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
In Vitro: 

DMSO : ≥ 100 mg/mL(199.69 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9969 mL9.9844 mL19.9688 mL
5 mM0.3994 mL1.9969 mL3.9938 mL
10 mM0.1997 mL0.9984 mL1.9969 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM，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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。