Sertaconazole nitrate 硝酸舍他康唑; FI7056|cas:99592-39-9|西域试剂

Sertaconazole nitrate 硝酸舍他康唑; FI7056,99.58%

产品编号：Bellancom-B0736A| CAS NO：99592-39-9| 分子式：C₂₀H₁₆Cl₃N₃O₄S| 分子量：500.78

Sertaconazole硝酸盐是局部广谱的抗真菌剂，可作用于表皮和粘膜的感染。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-B0736A	￥450.00	杭州北京（现货）
Bellancom-B0736A	￥750.00	杭州北京（现货）
Bellancom-B0736A	￥1200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Sertaconazole nitrate 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 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^[4].

体外研究

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.
Sertaconazole nitrate (1 µg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner.
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.
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.
Sertaconazole nitrate (20, 40 µM; 24 h) induces apoptosis through p53 pathway in HeLa cells.
Sertaconazole nitrate (20, 30 µM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner.
Sertaconazole nitrate (15, 30 µM; 24 h) induces autophagy in A549, H460 cells^[4].

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

Cell Viability Assay

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

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

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

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

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

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

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

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.

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

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

体内研究

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

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

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

体内研究

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

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

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

性状

Solid

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 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
10 mM	0.1997 mL	0.9984 mL	1.9969 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°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。

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-CD in 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 μL 20% 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西域网站选购。

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)

参考文献

. Carrillo-Muñoz AJ, et al. In-vitro antifungal activity of sertaconazole, econazole, and bifonazole against Candida spp. J Antimicrob Chemother. 1995 Oct;36(4):713-6. [Content Brief]

. Sur R, et al. Anti-inflammatory activity of sertaconazole nitrate is mediated via activation of a p38-COX-2-PGE2 pathway. J Invest Dermatol. 2008 Feb;128(2):336-44. [Content Brief]

. Sebastian J, et al. Sertaconazole induced toxicity in HeLa cells through mitotic arrest and inhibition of microtubule assembly. Naunyn Schmiedebergs Arch Pharmacol. 2021 Jun;394(6):1231-1249. [Content Brief]

[4]. Zhang W, et al. Sertaconazole provokes proapoptotic autophagy via stabilizing TRADD in nonsmall cell lung cancer cells. MedComm (2020). 2021 Dec 16;2(4):821-837. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

危险品运输编码	NONH for all modes of transport
海关编码	2934999090

1. 物质的识别

产品名：	Sertaconazole nitrate
CAS号：	99592-39-9
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Sertaconazole nitrate
别名：	FI-7045
分子式：	C20H15Cl3N2OS.HNO3
分子量：	500.78

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Liebel, F., et al., Anti-inflammatory and anti-itch activity of sertaconazole nitrate. Arch Dermatol Res, 2006. 298(4): p. 191-9.

[2]. Pfaller, M.A. and D.A. Sutton, Review of in vitro activity of sertaconazole nitrate in the treatment of superficial fungal infections. Diagn Microbiol Infect Dis, 2006. 56(2): p. 147-52.

[3]. Sur, R., et al., Anti-inflammatory activity of sertaconazole nitrate is mediated via activation of a p38-COX-2-PGE2 pathway. J Invest Dermatol, 2008. 128(2): p. 336-44.

Sertaconazole nitrate 硝酸舍他康唑; FI7056,99.58%

Sertaconazole nitrate 硝酸舍他康唑; FI7056

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

在线咨询