| 应用 |
A substrate competitive and tight-binding inhibitor of autotaxin. |
| 产品介绍 |
PF-8380是高活性的autotaxin特异性抑制剂，IC50为2.8 nM。 |
| 生化机理 |
PF-8380 is an orally bioavailable piperazinylbenzoxazolone compound that acts as a substrate competitive and tight-binding inhibitor of autotaxin activity {IC50 = 2.8 and 1.7 nM for recombinant human enzyme-β isoform employing FS-3 and LPC (lysophosphatidylcholine) as substrates, respectively; 1.16 and 1.15 nM for rat/murine enzyme-FS-3 and fetal fibroblast cell-LPC; 101 nM for human whole blood}. |
| 别名 |
PF 8380;PF8380; 4-[3-氧代-3-(2-氧代-2,3-二氢苯并恶唑-6-基)丙基]哌嗪-1-羧酸 3,5-二氯苄酯;PF 8380;PF8380;6-(3-(piperazin-1-yl)propanoyl)benzo(d)oxazol-2(3H)-one;4-[3-(2,3-Dihydro-2-oxo-6-benzoxazolyl)-3-oxopropyl]-1-piperazinecarboxylic acid (3,5-dichlorophenyl)methyl ester; 4-[3-Oxo-3-(2-oxo-2,3-dihydrobenzoxazol-6-yl)propyl]piperazine-1-carboxylic acid 3,5-dichlorobenzyl ester |
