1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE

1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE 화학적 특성, 용도, 생산

• 개요

  Antagonists of the chemotactic and inflammatory lipoxygenase product leukotriene B₄ (LTB₄) have been potential drug development targets for several years. 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. LY255283 exhibits IC₅₀ values of ~950 nM and >10 μM at human recombinant BLT₂ and BLT₁ receptors, respectively. 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.

• 용도

  LY-255283 is a selective, competitive BLT2 receptor antagonist used in the treatment of chronic myeloid leukemia.

• 생물학적 활성

  Selective, competitive antagonist of BLT 2 receptors (IC 50 values are ~ 1 and > 10 μ M at human recombinant BLT 2 and BLT 1 receptors respectively). Inhibits LTB 4 -induced contraction of lung parenchyma (pA 2 = 7.2), and reduces LTB 4 -mediated airway obstruction in guinea pigs following i.v. and oral administration.

1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE 공급 업체

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