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。
| 生物活性 | SC75741 is a broad and efficientNF-κBinhibitor with anIC50of 200 nM forp65[1]. SC75741 blocksinfluenza viruses (IV)replication. SC75741 impairs DNA binding of theNF-κBsubunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibitscaspaseactivation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2]. |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(147.31 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-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: ≥ 2.08 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
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