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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: 2-8℃，2 years
- 保质期：
Powder: 2-8℃，2 years
- 英文名：
C 87
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
332420-90-3
- 规格：
25mg/10mg/5mg/1mg
| 规格： | 25mg | 产品价格： | ￥2490.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1190.0 |
| 规格： | 5mg | 产品价格： | ￥790.0 |
| 规格： | 1mg | 产品价格： | ￥344.0 |
| 基本信息 | |
| CAS | No.332420-90-3 |
| 英文名称 | C 87 |
| 分子式 | C24H15ClN6O3S |
| 分子量 | 502.93 |
| 溶解性 | Soluble in DMSO ≥0.5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder: 2-8℃，2 years |
| SMILES | C1=CC=C(C=C1)C2=CSC(=N2)N3C(=O)C(=C(N3)C4=CC=CC=C4)N=NC5=CC(=C(C=C5)Cl)[N+](=O)[O-] |
| InChIKey | HTEQQWJUYYUNQG-UHFFFAOYSA-N |
| InChI | InChI=1S/C24H15ClN6O3S/c25-18-12-11-17(13-20(18)31(33)34)27-28-22-21(16-9-5-2-6-10-16)29-30(23(22)32)24-26-19(14-35-24)15-7-3-1-4-8-15/h1-14，29H |
| PubChem CID | 4016403 |
| 靶点 | TNF-α |
| 通路 | Apoptosis |
| 背景说明 | C 87是一种新型小分子 TNFα 抑制剂。 |
| 生物活性 | C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.[1] |
| IC50 | IC50: 8.73 μM (TNFα-induced cytotoxicity)[1] |
| In Vitro | To explore chemical inhibitors against TNFα activity， we applied computer-aided drug design combined with in vitro and cell-based assays and identified a lead chemical compound， (E)-4-(2-(4-chloro-3-nitrophenyl) (named as C87 thereafter)， which directly binds to TNFα， potently inhibits TNFα-induced cytotoxicity (IC50 = 8.73 μM) and effectively blocks TNFα-triggered signaling activities.Furthermore， by using a murine acute hepatitis model， we showed that C87 attenuates TNFα-induced inflammation， thereby markedly reducing injuries to the liver and improving animal survival.[1]。 |
| 细胞实验 | By using a murine acute hepatitis model， we showed that C87 attenuates TNFα - induced inflammation， thereby markedly reducing injuries to the liver and improving animal survival.[1]。 |
| 细胞实验 | The inhibition of the cytotoxic effect of human TNFα by compounds (C 87) is measured in L929 cell line. L929 cells are seeded at a density of 104 cells/well in a 96-well plate and incubated for 24 h in RPMI 1640 with 10% FBS at 37°C. Compounds (C 87) are added to the cells with 1 μg/mL actinomycin D and 1 ng/mL TNFα and then incubated at 37 °C for 20 h before analysis. Cell survival is measured using the MTT method[1]. |
| 动物实验 | BALB/c mice are used in the study. Before LPS/GalN challenge (LPS (50 μg/kg) and D-GalN (1.2g/kg))， mice are injected intraperitoneally with C 87 (12.5 mg/kg)， Enbrel (4 mg/kg)， or vehicle， respectively， at 1， 8， and 16 h. Blood is collected with retro-orbital sampling. Activities of alanine transaminase and aspartate transaminase are detected. Liver tissues are collected and fixed in 10% formalin， and sections are stained with hematoxylin and eosin[1]. |
| 数据来源文献 | [1]. Ma L， et al. A novel small-molecule tumor necrosis factor α inhibitor attenuates inflammation in a hepatitis mouse model. J Biol Chem. 2014 May 2;289(18):12457-66. |
| 单位 | 瓶 |
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