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 Basic information
- Product Name:
- 1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE
- Synonyms:
-
- LY 255283
- 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-TETRAZOLE-5-YL)HEPTYL]OXY]PHENYL]-ETHANONE
- 5'-Ethyl-2'-hydroxy-4'-[6-methyl-6-(1H-tetrazol-5-yl)heptyloxy]acetophenone
- CGS 23356
- 1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone
- Ethanone, 1-[5-ethyl-2-hydroxy-4-[[6-methyl-6-(2H-tetrazol-5-yl)heptyl]oxy]phenyl]-
- 1-(5-Ethyl-2-hydroxy-4-((6-methyl-6-(2H-tetrazol-5-yl)heptyl)oxy)phenyl)ethan-1-one
- CAS:
- 117690-79-6
- MF:
- C19H28N4O3
- MW:
- 360.45
- Product Categories:
-
- Prostanoid receptor and related
- Mol File:
- 117690-79-6.mol
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE Chemical Properties
- Melting point:
- 160-162 °C
- Boiling point:
- 573.4±60.0 °C(Predicted)
- Density
- 1.157±0.06 g/cm3(Predicted)
- storage temp.
- Store at +4°C
- solubility
- DMSO: >20mg/mL
- pka
- 5.11±0.10(Predicted)
- form
- powder
- color
- off-white to light yellow
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONE Usage And Synthesis
Description
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.
Uses
LY-255283 is a selective, competitive BLT2 receptor antagonist used in the treatment of chronic myeloid leukemia.
Definition
ChEBI: 1-[5-ethyl-2-hydroxy-4-[6-methyl-6-(2H-tetrazol-5-yl)heptoxy]phenyl]ethanone is an aromatic ketone.
Biological Activity
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.
storage
Store at +4°C
1-[5-ETHYL-2-HYDROXY-4-[[6-METHYL-6-(1H-TETRAZOL-5-YL)HEPTYL]OXY]PHENYL]ETHANONESupplier
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