| Identification | Back Directory | [Name]
LY 223982 | [CAS]
117423-74-2 | [Synonyms]
CGS23131
LY 223982
SKF107324)
LY223982 Exclusive
SYZSSLLFRVDRHL-QPJJXVBHSA-N
LY223982 (Synonyms: CGS23131
5-(3-Carboxybenzoyl)-2-[(E)-6-(4-methoxyphenyl)-5-hexenyloxy]benzenepropanoic acid
Benzenepropanoic acid, 5-(3-carboxybenzoyl)-2-[[(5E)-6-(4-methoxyphenyl)-5-hexen-1-yl]oxy]- | [Molecular Formula]
C30H30O7 | [MDL Number]
MFCD00876442 | [MOL File]
117423-74-2.mol | [Molecular Weight]
502.55 |
| Chemical Properties | Back Directory | [Melting point ]
151-152 °C | [Boiling point ]
753.8±60.0 °C(Predicted) | [density ]
1.235±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C Freezer | [solubility ]
Chloroform (Slightly, Heated, Sonicated), DMSO (Very Slightly) | [form ]
A crystalline solid | [pka]
3.81±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and is an important mediator of the inflammatory process. The benzophenone dicarboxylic acid derivative LY223982 is a potent BLT1 receptor antagonist. It inhibits the specific binding of radiolabeled-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM. LY223982 inhibits the leukotriene B4 (LTB4)-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively. However, concentrations of LY223982 up to 10 μM do not inhibit binding of LTB4 to human BLT1 or BLT2 expressed in CHO cells. | [Uses]
LY223982 is a potent P2Y7 (BLT1) receptor antagonist. | [in vivo]
LY223982 inhibits transient leukopenia induced in rabbits with LTB4 (ED50, 3 mg/kg) but not with FMLP, and shows no agonist activity in any of the test systems[1]. | [IC 50]
LTB4: 13.2 nM (IC50) | [storage]
Store at -20°C | [References]
[1] D. MARK GAPINSKI. Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain[J]. Journal of Medicinal Chemistry, 1990, 33 10: 2807-2813. DOI: 10.1021/jm00172a020
[2] W T JACKSON. Specific inhibition of leukotriene B4-induced neutrophil activation by LY223982.[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263 3: 1009-1014.
[3] T. YOKOMIZO. Hydroxyeicosanoids Bind to and Activate the Low Affinity Leukotriene B4 Receptor, BLT2*[J]. The Journal of Biological Chemistry, 2001, 3 1: 12454-12459. DOI: 10.1074/jbc.m011361200 |
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