store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release.
ターゲット&IC50 | LTB4:250±85 nM |
In vitro | Bunaprolast (U-66,858) is metabolized through deacetylation to produce an initial metabolite, U-68,244, which retains similar pharmacologic efficacy. This study focuses on their ability to inhibit the ionophore-induced production of leukotriene B4 (LTB4) in human whole blood (WB). Pre-treatment with Bunaprolast or U-68,244 for one minute before exposure to calcium ionophore A23187 yields inhibition concentrations (IC50s) of 1080±644 nM and 820±442 nM respectively, which improve to 250±85 nM and 270±79 nM after 60 minutes. This inhibitory effect is comparable to the lipoxygenase inhibitor AA-861, whereas vitamin K and Bunaprolast's sulfate conjugate only inhibit LTB4 release at higher micromolar levels. Additionally, Bunaprolast significantly reduces thromboxane A2 release (p<0.02) compared to the cyclooxygenase (CO) inhibitor Flurbiprofen, underscoring its potential as a therapeutic agent. |
別名 | U66858 |
分子量 | 272.34 |
分子式 | C17H20O3 |
CAS No. | 99107-52-5 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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Bunaprolast 99107-52-5 Immunology/Inflammation Metabolism Lipoxygenase LTR U-66858 U 66858 U66858 Inhibitor inhibitor inhibit