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Bunaprolast

Catalog No. T17191 CAS 99107-52-5

Synonyms: U66858

Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release.

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Bunaprolast, CAS 99107-52-5

Pack Size	Availability	Price/USD	Quantity
1 mg	In stock	$ 700.00
5 mg	In stock	$ 1,800.00

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Purity: 99.9%

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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

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Johnson HG, et al. Activity of a novel hydroquinone inhibitor of leukotriene synthesis (U-66,858) in the rhesus monkey Ascaris reactor. Int Arch Allergy Appl Immunol. 1988;87(2):204-7. 2. Summers JA, et al. Lipoxygenase inhibitory activity of U-66,858 and its deacetylated metabolite U-68,244 in human whole blood. Agents Actions. 1994 Mar;41(1-2):32-6.

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Keywords

Bunaprolast 99107-52-5 Immunology/Inflammation Metabolism Lipoxygenase LTR U-66858 U 66858 U66858 inhibitor inhibit

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