| 产品描述： | Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor |
| 靶点： |
COX-1:3.9 μM (IC50);COX-2:8.1 μM (IC50);Caspase-1:4.4 μM (IC50);Caspase-3:1.2 μM (IC50);Caspase-4:0.57 μM (IC50);Caspase-5:0.87 μM (IC50);Caspase-9:0.76 μM (IC50);ATPase;Caspase;COX |
| 体外研究： |
Fenbufen (100-500 μM) improves the viability of apoptotic THP-1 cells treated with 25 μM Nigericin (HY-127019) |
| 体内研究： |
Fenbufenmay (1200 mg/kg; feed) does not cause gastric ulceration whilst inducing a near maximal inhibition of prostaglandin release in rats. Fenbufenmay (1200 mg/kg; p.o.; diet; for 10 days) blocks the hypertrophy of the heart but not that of the skeletal muscles. Animal Model: Male hooded Lister rats Dosage: 1200 mg/kg Administration: Oral administration, diet, for 10 days Result: Significantly reduced Clenbuterol (2mg/kg)-induced hypertrophy of the heart. |
| 参考文献： |
1. A E Sloboda, et al. The pharmacological properties of fenbufen. A review. Arzneimittelforschung. 1980;30(4A):716-21. 2. R G Child, et al. Fenbufen, a new anti-inflammatory analgesic: synthesis and structure-activity relationships of analogs, J Pharm Sci. 1977 Apr;66(4):466-76. 3. A E Sloboda, et al. The pharmacology of fenbufen, 3-(4-biphenylylcarbonyl)propionic acid, and 4-biphenylacetic acid, interesting antiinflammatory-analgesic agents. Inflammation. 1976 Dec;1(4):415-38. 4. Asif Husain, et al. Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents. Eur J Med Chem . 2009 Sep;44(9):3798-804. 5. Christina E Smith, et al. Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors. Cell Chem Biol. 2017 Mar 16;24(3):281-292. 6. R M Palmer, et al. Effects of the cyclo-oxygenase inhibitor, fenbufen, on clenbuterol-induced hypertrophy of cardiac and skeletal muscle of rats. Br J Pharmacol. 1990 Dec;101(4):835-8. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.933 ml |
19.663 ml |
39.327 ml |
| 5 mM |
0.787 ml |
3.933 ml |
7.865 ml |
| 10 mM |
0.393 ml |
1.966 ml |
3.933 ml |
| 50 mM |
0.079 ml |
0.393 ml |
0.787 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京