C 87
目录号 : GC33826
C87是一种新型小分子TNFα抑制剂;高效抑制TNFα诱导的细胞毒性，IC50值为8.73μM。
Cas No.:332420-90-3
Sample solution is provided at 25 µL, 10mM.
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C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
C87 directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50=8.73 μM) and effectively blocks TNFα-triggered signaling activities. C87 exhibits good solubility and consistent dose-dependent functions in vitro. C87 completely blocks TNFα-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C87 in L929 cells. C87 also prevents the degradation of IκBα in cells treated with TNFα. C87 potently blocks multiple signaling transduction pathways and downstream target gene activation triggered by TNFα[1].
C87 attenuates TNFα-induced inflammation, thereby markedly reducing injuries to the liver and improving animal survival. C87 injection delays the incidence of death and increases the survival rate by two folds compared with the vehicle control. The level of alanine transaminase and aspartate transaminase is consistently reduced in mice with C87 treatment[1].
[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.
Cell experiment: | The inhibition of the cytotoxic effect of human TNFα by compounds (C87) 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 (C87) 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]. |
Animal experiment: | 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 C87 (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]. |
References: [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. | |
| Cas No. | 332420-90-3 | SDF | |
| Canonical SMILES | O=C(N(C1=NC(C2=CC=CC=C2)=CS1)N=C/3C4=CC=CC=C4)C3=N\NC5=CC=C(Cl)C([N+]([O-])=O)=C5 | ||
| 分子式 | C24H15ClN6O3S | 分子量 | 502.93 |
| 溶解度 | DMSO : 9.33 mg/mL (18.55 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store 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 | 1.9883 mL | 9.9417 mL | 19.8835 mL |
| 5 mM | 0.3977 mL | 1.9883 mL | 3.9767 mL |
| 10 mM | 0.1988 mL | 0.9942 mL | 1.9883 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