LY-255283A selective, competitive BLT2 receptor antagonist

LY-255283 (CAS 117690-79-6)

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Synonym: 1-[5-Ethyl-2-hydroxy-4-[[6-methyl-6-(1H-tetrazol-5-yl)heptyl]oxy]phenyl]ethanone
Application: A selective, competitive BLT2 receptor antagonist
CAS Number: 117690-79-6
Purity: 98%
Molecular Weight: 360.5
Molecular Formula: C19H28N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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LY-255283 is a hydroxyacetophenone that acts as a leukotriene B4 receptor antagonist. Specifically, LY-255283 competes with LTB4 (sc-201043) and [3H]LTB4 to bind to the P2Y7 (BLT1) and LTB4R2 (BLT2) receptor on lung cell membranes. Studies show that the binding coefficient of LY-255283 is smaller than LTB4, resulting in a weaker bond between the receptor and the antagonist. In addition, LY-255283 competitively reduces the contractile responses of lung parenchyma that are caused by the binding of LTB4 to the receptor. LY-255283 is an inhibitor of LTB4R2.


References

1. Richards, I.M., et al. 1991. Ann. N. Y. Acad. Sci. 629: 274-287. PMID: 1659282
2. Taylor, B.M., et al. 1991. Prostaglandins. 42: 211-224. PMID: 1664113
3. Silbaugh, S.A., et al. 1992. Eur. J. Pharmacol. 223: 57-64. PMID: 1335877
4. Herron, D.K., et al. 1992. J. Med. Chem. 35: 1818-1828. PMID: 1316967
5. Souza, D.G., et al. 2000. Eur. J. Pharmacol. 403: 121-128. PMID: 10969152
6. Yokomizo, T., et al. 2001. J. Biol. Chem. 276: 12454-12459. PMID: 11278893

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (25 mM), DMF (50 mg/ml), water (0.1 mgml) at 25° C, and 1:1 solution of DMF : PBS (pH 7.2) (100 µg/ml).
Storage :
Store at -20° C
Melting Point :
221.5° C (Predicted)
Boiling Point :
~573.4° C at 760 mmHg (Predicted)
Density :
1.16 g/cm3
Refractive Index :
n20D 1.55
IC50 :
BLT2 receptors: IC50 = ~1 µM (human); BLT1 receptors: IC50 = >10 µM (human); radiolabeled LTB4: IC50 = 100 nM (guinea pig lung membrane); the binding of radiolabeled LTB4 to eosinophil membranes: IC50 = 260 nM
Ki Data :
Leukotriene B4 receptor 1: Ki= 77 nM (human); Leukotriene B4 receptor 2: Ki= 78 nM (human)
pK Values :
pKa: 5.52, pKb: 1.50
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
PubChem CID :
122023
MDL Number :
MFCD00876422
SMILES :
CCC1=C(C=C(C(=C1)C(=O)C)O)OCCCCCC(C)(C)C2=NNN=N2

Download SDS (MSDS)

Certificate of Analysis

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