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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

LY255283

Cayman Chemical Item Number 70715

(CAS 117690-79-6)

LY255283 (CAS 117690-79-6)

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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%
λmax 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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LY255283 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $19.00 $0.00
5 mg $76.00 $0.00
10 mg $114.00 $0.00
25 mg $214.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

Related Products

BLT2 Receptor Blocking Peptide
BLT2 Receptor Polyclonal Antibody
Leukotriene B4
Leukotriene B4 dimethyl amide
U-75302
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