SC75741

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SC75741  纯度: 99.51%

SC75741 是一种广泛，有效的 NF-κB 抑制剂，对 p65 的 IC50 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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