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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 700.00 | |
5 mg | In stock | $ 1,800.00 |
Description | Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release. |
Targets&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. |
In vivo | The IgE-mediated hypersensitivity to Ascaris antigen in reactor rhesus primates is used to assess the pharmacologic profile of Bunaprolast (U-66,858). When given orally, Bunaprolast shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes. When administered via aerosol, it exhibits dose-independent inhibition. In 15 animals receiving aerosols (52±32 to 53±10% for RL, p=0.05, and 45±19 to 28±19% Cdyn inhibitions, p=0.05) at concentrations ranging from 5.0% to 0.1%, Bunaprolast demonstrates significant effects. By the oral route, inhibition is observed at 1-4 h following administration. In 5 animals, oral doses of 10 and 5 mg/kg result in inhibition (RL by 98±2 to 78±1.5%, p=0.01, and Cdyn by 75±17 to 60.9±9.1%, p=0.05) for 10 and 5 mg/kg of Bunaprolast, respectively[1]. |
Synonyms | U66858 |
Molecular Weight | 272.34 |
Formula | 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. More
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Bunaprolast 99107-52-5 Immunology/Inflammation Metabolism Lipoxygenase LTR U-66858 U 66858 U66858 inhibitor inhibit