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SC75741

现货
Catalog No.
B4749
NF-κB抑制剂
组合的产品项目
规格价格库存 数量
50mg
¥ 5,510.00
现货
10mg
¥ 1,370.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt565.67
Cas No.913822-46-5
FormulaC29H23N7O2S2
Solubility≥37.6 mg/mL in DMSO, <2.86 mg/mL in H2O, ≥12.56 mg/mL in EtOH with ultrasonic and warming
Chemical Name(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
SDFDownload SDF
Canonical SMILESO=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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

上皮Madin-Darbycanine肾细胞(MDCK)

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM、2 μM或5 μM,24 h

应用

在上皮Madin-Darbycanine肾细胞(MDCK)中,SC75741以剂量依赖性方式抑制病毒繁殖。SC75741(5 μM)处理MDCK细胞抑制单环和多环感染中的病毒复制,在A型和B型流感病毒感染复制的较后阶段具有最高功效。SC75741对H1N1和H3N2甲型流感病毒亚型和乙型流感病毒复制表现出抗病毒活性。在人肺泡II型上皮细胞系A549中,SC75741以浓度依赖性方式有效降低后代病毒滴度。SC75741(55小时和65小时)延长治疗以浓度依赖的方式降低细胞活力。SC75741(5 μM)抑制NF-κB依赖性基因的转录激活。SC75741(5 μM)降低了病毒诱导的NF-kB靶基因IL-6和TRAIL的表达,但不抑制IFN-b或IRF-3活性。SC75741(5 μM)对抗性病毒变异体发展具有高度障碍作用。

动物实验 [1]:

动物模型

C57BL/6小鼠

给药剂量

腹腔注射,15 mg/kg

应用

SC75741 (15 mg/kg, i.p.)降低H5N1流感病毒感染后小鼠肺部的病毒复制和细胞因子表达。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

生物活性

Description SC75741是一种有效的NF-κB抑制剂,EC50值为200 nM.
靶点 NF-κB          
IC50 200 nM          

质量控制

化学结构

SC75741