C 87
Based on 2 publication(s) in Google Scholar
C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
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- 純度: 98.16%
- CAS 番号: 332420-90-3
- 分子式: C24H15ClN6O3S
- 分子量:502.93
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 C 87
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生物活性
IC50: 8.73 μM (TNFα-induced cytotoxicity)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | CC50 |
10.81 μM
Compound: C87
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Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 33479624] |
| THP-1 | IC50 |
0.11 μM
Compound: C87
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Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
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[PMID: 33479624] |
C 87 (C87) directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50=8.73 μM) and effectively blocks TNFα-triggered signaling activities. C 87 exhibits good solubility and consistent dose-dependent functions in vitro. C 87 completely blocks TNFα-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C 87 in L929 cells. C 87 also prevents the degradation of IκBα in cells treated with TNFα. C 87 potently blocks multiple signaling transduction pathways and downstream target gene activation triggered by TNFα[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 332420-90-3
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性状 Solid
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分子量 502.93
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分子式 C24H15ClN6O3S
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Color Yellow to orange
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Eur J Immunol
Fibroblast transdifferentiation promotes conversion of M1 macrophages and replenishment of cardiac resident macrophages following cardiac injury in mice. [Abstract]2020 Jun;50(6):795-808. PMID: 32068249 -
J Immunol
β-Arrestin 2 Regulates Inflammatory Responses against Mycobacterium tuberculosis Infection through ERK1/2 Signaling. [Abstract]2021 Jun 1;206(11):2623-2637. PMID: 34001657
溶剤 & 溶解度
DMSO : 5.05 mg/mL (10.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 15% Solutol HS 15 10% Cremophor EL 35% PEG400 40% Water
Solubility: 2 mg/mL (3.98 mM); Suspended solution; Need ultrasonic
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9883 mL | 9.9417 mL | 19.8835 mL | 49.7087 mL |
| 5 mM | 0.3977 mL | 1.9883 mL | 3.9767 mL | 9.9417 mL | |
| 10 mM | 0.1988 mL | 0.9942 mL | 1.9883 mL | 4.9709 mL |
C 87 関連分類
HY-100735 関連分類
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