Product Details
| Product Name:
Bunaprolast |
CAS No.:
99107-52-5 |
| Purity:
99.9% |
Supply Ability:
10g |
| Release date:
2024/11/20 |
Product Introduction
Bioactivity
| Name | Bunaprolast |
| Description | Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release. |
| 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 utilized to evaluate the pharmacologic profile of Bunaprolast (U-66,858). Oral administration of Bunaprolast shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes, while aerosol administration results in dose-independent inhibition. In 15 animals receiving aerosols (52±32 to 53±10% inhibition for RL, p=0.05, and 45±19 to 28±19% inhibition for Cdyn, p=0.05) at concentrations from 5.0% to 0.1%, Bunaprolast demonstrates significant effects. Orally, inhibition is observed 1-4 hours post-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]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Keywords | U-66858 | U 66858 | Bunaprolast |
| Inhibitors Related | 2,5-Di-tert-butylhydroquinone | Montelukast sodium | Caffeic Acid | 5-LOX inhibitor | Diethylcarbamazine citrate | Resveratrol | NNK | 5-Aminosalicylic Acid | Malotilate | Bestatin |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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