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Cat. No.: HY-U00170

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Bunaprolast

(Synonyms: U66858)

Bunaprolast (U66858) is a potent inhibitor of LTB₄ production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB₂ release.

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CAS No.: 99107-52-5
화학식: C₁₇H₂₀O₃
분자량:272.34

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

Bunaprolast Chemical Structure

CAS No.: 99107-52-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

Bunaprolast (U66858) is a potent inhibitor of LTB₄ production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB₂ release.

IC₅₀ & Target^[1]

LTB₄

TXB₂

5-LO

All Leukotriene Receptor Isoforms :

All Prostaglandin Receptor Isoforms :

All Lipoxygenase Isoforms :

In Vitro

Bunaprolast (U-66,858) undergoes deacetylation to an initial metabolite with similar pharmacological potency. The inhibitory effects of the semi-quinone Bunaprolast and its metabolite U-68,244 on the ionophore-induced formation of leukotriene B4 (LTB4) are examined in human whole blood (WB). Preincubation of Bunaprolast and U-68,244 for 1 min prior to challenge of blood with calcium ionophore A23187 results in IC₅₀s of 1080±644 and 820±442 nM, respectively. After 60 min preincubation, IC₅₀s are 250±85 and 270±79 nM. The activity of the lipoxygenase inhibitor AA-861 in this system is similar to that of Bunaprolast, while vitamin K and the sulphate conjugate of Bunaprolast show significant inhibition of LTB4 release only at micromolar concentrations. Bunaprolast exhibits significant inhibition of thromboxane A2 release (p<0.02) in a comparative study with the known cyclooxygenase (CO) inhibitor Flurbiprofen^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 Bunaprolast is given by the oral route, it shows dose-related inhibition of resistance (RL) and compliance (Cdyn) changes. When Bunaprolast is given by the aerosol route, it shows dose independent inhibition. In 15 animals, aerosols (52±32 to 53±10% for RL, p=0.05 and 45±19 to 28±19% Cdyn inhibitions, p=0.05) for 5.0-0.1% aerosol. By the oral route, inhibition is seen at 1-4 h following administration. In 5 animals, oral doses of 10 and 5 mg/kg inhibit (RL by 98±2 to 78±1.5%, p=0.01 and Cdyn by 75±17 to 60.9±9.1%, p=0.05) by 10 and 5 mg/kg Bunaprolast, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 99107-52-5
분자량 272.34
화학식 C₁₇H₂₀O₃
SMILES

COC1=C2C=CC=CC2=C(OC(C)=O)C(CCCC)=C1
Synonyms

U66858
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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Bunaprolast

All Leukotriene Receptor Isoforms

All Prostaglandin Receptor Isoforms

All Lipoxygenase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

Bunaprolast Related Classifications

HY-U00170 Related Classifications