C 87 |
| Catalog No.GC33826 |
C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 332420-90-3
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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 | ||
| Formula | C24H15ClN6O3S | M.Wt | 502.93 |
| Solubility | DMSO : 9.33 mg/mL (18.55 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *