LY255283 (CAS 117690-79-6) || Cayman Chemical

LY255283

Cayman Chemical Item Number 70715

(CAS 117690-79-6)

LY255283 (CAS 117690-79-6)

Description

Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B₄ (LTB₄) have been potential drug development targets for several years.^1,2 The tetrazole LY255283 is a competitive antagonist of the BLT₂ receptor. It displaces radiolabeled LTB₄ from guinea pig lung membrane, with an IC₅₀ of about 100 nM.³ LY255283 exhibits IC₅₀ values of ~950 nM and >10 µM at human recombinant BLT₂ and BLT₁ receptors, respectively.⁴ LY255283 inhibits eosinophil chemotaxis by 80% at a concentration of 10 µM, and inhibits the binding of radiolabeled LTB₄ to eosinophil membranes with an IC₅₀ of 260 nM.¹

1 Richards, I.M., Sun, F.F., Taylor, B.M., et al. Contribution of leukotriene B₄ to airway inflammation and the effect of antagonists. Ann N Y Acad Sci 629 274-287 (1991).

2 Taylor, B.M., Crittenden, N.J., Bruden, M.N., et al. Biological activity of leukotriene B₄ analogs: Inhibition of guinea pig eosinophil migration in vitro by 2,6-disubstituted pyridine analogs U-75,302 and U-75,485. Prostaglandins 42 211-224 (1991).

3 Silbaugh, S.A., Stengel, P.W., Cockerham, S.L., et al. Pulmonary actions of LY255283, a leukotriene B₄ receptor antagonist. Eur J Pharmacol 223 57-64 (1992).

4 Yokomizo, T., Kato, K., Hagiya, H., et al. Hydroxyeicosanoids bind to and activate the low affinity leukotriene B₄ receptor, BLT₂. J Biol Chem 276(15) 12454-12459 (2001).

Formal Name

1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(1H-tetrazol-5-yl)heptyl]oxy]phenyl]-ethanone

CAS Number

117690-79-6

Molecular Formula

C₁₉H₂₈N₄O₃

Formula Weight

360.5

Formulation

A crystalline solid

Purity

>98%

λ_max

213, 232, 276, 326 nm

Stability

1 year

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

SMILES

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CCc1c(OCCCCCC(C)(C)c2nnn[nH]2)cc(O)cc1C(=O)C

Background Reading

Richards, I.M., Sun, F.F., Taylor, B.M., et al. Contribution of leukotriene B₄ to airway inflammation and the effect of antagonists. Ann N Y Acad Sci 629 274-287 (1991).

Taylor, B.M., Crittenden, N.J., Bruden, M.N., et al. Biological activity of leukotriene B₄ analogs: Inhibition of guinea pig eosinophil migration in vitro by 2,6-disubstituted pyridine analogs U-75,302 and U-75,485. Prostaglandins 42 211-224 (1991).

Yokomizo, T., Kato, K., Hagiya, H., et al. Hydroxyeicosanoids bind to and activate the low affinity leukotriene B₄ receptor, BLT₂. J Biol Chem 276(15) 12454-12459 (2001).

Silbaugh, S.A., Stengel, P.W., Cockerham, S.L., et al. Pulmonary actions of LY255283, a leukotriene B₄ receptor antagonist. Eur J Pharmacol 223 57-64 (1992).

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