SC75741

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SC75741  纯度: 99.51%

SC75741 是一种广泛,有效的 NF-κB 抑制剂,对 p65IC50 为 200 nM。SC75741 可阻断 influenza viruses 复制。SC75741 通过损害 NF-κB 亚基 p65 的 DNA 结合,导致细胞因子,趋化因子和促凋亡因子的表达降低,抑制 caspase 活化和阻断 caspase 介导的病毒核糖核蛋白 (viralribonucleoproteins) 的核输出。

SC75741

SC75741 Chemical Structure

CAS No. : 913822-46-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1120 In-stock
5 mg ¥900 In-stock
10 mg ¥1600 In-stock
25 mg ¥3100 In-stock
50 mg ¥5600 In-stock
100 mg ¥9900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].

IC50 & Target

p65

200 nM (IC50)

体外研究
(In Vitro)

SC75741 (5 μM; 24-96 hours) inhibits long-term A549 cells proliferation[2].
SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect for A549 cells within a time frame of about 50 and 65 hours[2].
SC75741 (5 μM; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 24, 48, 72 and 96 hours
Result: Inhibited long-term cell proliferation

Cell Viability Assay[2]

Cell Line: A549 cells
Concentration: 1, 2, 5 or 10 μM
Incubation Time: 5.5, 29, 50, 65 hours
Result: Reduced cells viability in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: MDCK cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Inhibited cleavage of the effector caspase 3 induced upon H7N7-infection.

体内研究
(In Vivo)

SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virus mRNA by 90% in the lungs of infected mice[2].
The plasma-levels of SC74751 (intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; for 3.5 and 6 hours) after i.v. administration decreases mono-exponentially and half-life is roughly 40 min. After i.p. administration, elimination of SC75741 seems to be limited by a slow uptake from the peritoneum and a half-life of 55 min is observed[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[2]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; for 2 days
Result: Reduced the amount of viral mRNA by 90%.
Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[1]
Dosage: 5 mg/kg or 15 mg/kg
Administration: Intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; 3.5 and 6 hours
Result: Half-life was roughly 40 min and 55 min for i.v. and i.p. administration, respectively.

分子量

565.67

Formula

C29H23N7O2S2

CAS 号

913822-46-5

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (147.31 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7678 mL 8.8391 mL 17.6782 mL
5 mM 0.3536 mL 1.7678 mL 3.5356 mL
10 mM 0.1768 mL 0.8839 mL 1.7678 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。-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: ≥ 2.08 mg/mL (3.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.68 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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: 2.08 mg/mL (3.68 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.68 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 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: ≥ 2.08 mg/mL (3.68 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.68 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 20.8 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Haasbach E, et al. The NF-kappaB inhibitor SC75741 protects mice against highly pathogenic avian influenza A virus. Antiviral Res. 2013 Sep;99(3):336-44.

    [2]. Ehrhardt C, et al. The NF-κB inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance. Cell Microbiol. 2013 Jul;15(7):1198-211.

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