详情描述
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.
Product information
CAS Number: 36330-85-5
Molecular Weight: 254.28
Formula: C16H14O3
Synonym:
CL-82204
Chemical Name: 4-{[1, 1'-biphenyl]-4-yl}-4-oxobutanoic acid
Smiles: OC(=O)CCC(=O)C1C=CC(=CC=1)C1C=CC=CC=1
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (196.63 mM; Need ultrasonic) H2O : 0.67 mg/mL (2.63 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Fenbufen (100-500 μM) improves the viability of apoptotic THP-1 cells treated with 25 μM Nigericin (HY-127019).
In Vivo:
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.
References:
- A E Sloboda, et al. The pharmacological properties of fenbufen. A review. Arzneimittelforschung. 1980;30(4A):716-21.
- 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.
- 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.
- 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.
Products are for research use only. Not for human use.