CAS |
No.36330-85-5 |
中文名称 |
芬布芬 |
英文名称 |
Fenbufen |
别名 |
Lederfen;CL-82204 |
分子式 |
C16H14O3 |
分子量 |
254.28 |
溶解性 |
Soluble in DMSO(Need ultrasonic) |
纯度 |
≥98% |
外观(性状) |
Solid |
储存条件 |
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
MDL |
MFCD00056701 |
SMILES |
C1=CC=C(C=C1)C2=CC=C(C=C2)C(=O)CCC(=O)O |
InChIKey |
ZPAKPRAICRBAOD-UHFFFAOYSA-N |
InChI |
InChI=1S/C16H14O3/c17-15(10-11-16(18)19)14-8-6-13(7-9-14)12-4-2-1-3-5-12/h1-9H,10-11H2,(H,18,19) |
PubChem CID |
3335 |
靶点 |
Others |
通路 |
Others |
背景说明 |
Fenbufen是一种苯基链烷衍生物,具有抗炎、止痛、解热的活性。 |
生物活性 |
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[1][2][3][4][5]. |
In Vitro |
Fenbufen (100-500 μM) improves the viability of apoptotic THP-1 cells treated with 25 μM Nigericin (HY-127019)[5]. |
In Vivo |
Fenbufenmay (1200 mg/kg; feed) does not cause gastric ulceration whilst inducing a near maximal inhibition of prostaglandin release in rats[6].Fenbufenmay (1200 mg/kg; p.o.; diet; for 10 days) blocks the hypertrophy of the heart but not that of the skeletal muscles[6].Animal Model: Male hooded Lister rats[6]:Dosage:1200 mg/kg;Administration:Oral administration, diet, for 10 days;Result:Significantly reduced Clenbuterol (2mg/kg)-induced hypertrophy of the heart. |
数据来源文献 |
[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. |
规格 |
100mg |
单位 |
瓶 |