SC75741
目录号 : GC10088
An inhibitor of NF-κB
Cas No.:913822-46-5
Sample solution is provided at 25 µL, 10mM.
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SC75741 is a potent NF-κB inhibitor with EC50 value of 200 nM.
NF-kB is a protein complex that regulates the expression of immunoreceptors, inflammatory cytokines and chemokines and is commonly regarded as a major antiviral factor. However, it has been shown that influenza A viruses exploit this signaling pathway for efficient replication [1].
In MDCK cells, inhibitory potential of 5 uM SC75741 on virus replication is highest at later stages of infection. In the human alveolar type II epithelial cell line A549 infected with H5N1 and H7N7 viruses, SC75741 provoked an efficient reduction of virus titers in a dose-dependent way [1].
In the lung of infected mice, SC75741 reduces viral replication and H5N1-induced IL6 and IP-10 expression. In addition, SC75741 also reduced cytokine production in vivo that is involved in hypercytokinemia mediated by influenza virus infection. Importantly, SC75741 exhibits a high barrier for virus variants [1].
References:
[1]. Ehrhardt C, Rückle A, Hrincius ER, 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, 15(7): 1198-1211.
| Cell experiment [1]: | |
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Cell lines |
Epithelial Madin–Darbycanine kidney cells (MDCK) |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1 μM, 2 μM or 5 μM, 24 h |
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Applications |
In Epithelial Madin–Darbycanine kidney cells (MDCK), SC75741 dose-dependently inhibited virus propagation. Treatment of MDCK cells with SC75741 (5 μM) inhibited virus replication in mono- and multicyclic infections with highest efficiency at later stages of infection replication of influenza A and B viruses. SC75741 exhibited antiviral activity on H1N1 and H3N2 influenza A virus subtype and influenza B virus replication. In the human alveolar type II epithelial cell line A549, SC75741 provoked an efficient reduction of progeny virus titres in a concentration-dependent manner. Prolonged treatment with SC75741 (55 h and 65 h) reduced cell viability in a concentration-dependent manner. SC75741 (5 μM) inhibited transcriptional activation of NF-kB-dependent genes. SC75741 (5 μM) reduced virus-induced expression of the NF-kB target genes IL-6 and TRAIL but not IFN-b or IRF-3 activity. SC75741 (5 μM) showed a high barrier for development of resistant virus variants. |
| Animal experiment [1]: | |
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Animal models |
C57BL/6 mice |
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Dosage form |
Intraperitoneal administration, 15 mg/kg |
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Application |
SC75741 (15 mg/kg, i.p.) reduced virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Ehrhardt C, Rückle A, Hrincius E R, et al. The NF‐κB inhibitor SC75741 efficiently blocks influenza virus propagation and confers a high barrier for development of viral resistance[J]. Cellular microbiology, 2013, 15(7): 1198-1211. |
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| Cas No. | 913822-46-5 | SDF | |
| 化学名 | (Z)-N-(6-benzoyl-1H-benzo[d]imidazol-2-yl)-2-(1-(thieno[3,2-d]pyrimidin-4-yl)piperidin-4-yl)thiazole-4-carbimidic acid | ||
| Canonical SMILES | O=C(C1=CC2=C(N=C(/N=C(O)/C3=CSC(C4CCN(C5=NC=NC6=C5SC=C6)CC4)=N3)N2)C=C1)C7=CC=CC=C7 | ||
| 分子式 | C29H23N7O2S2 | 分子量 | 565.67 |
| 溶解度 | ≥ 37.6 mg/mL in DMSO, ≥ 12.56 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Desiccate at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet