LY 171883A selective leukotriene D4 antagonist

LY 171883 (CAS 88107-10-2)

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Application: A selective leukotriene D4 antagonist
CAS Number: 88107-10-2
Molecular Weight: 318.4
Molecular Formula: C16H22N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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LY 171883, a CysLT1 Receptor (leukotriene D4) antagonist, has been shown to displace oleic acid (sc-200797) binding to fatty-acid-binding protein (FABP) which may be involved in fatty acid metabolism. Studies suggest that this compound contains structural similarity to fatty acids, hence the ability to bind to FABPs. Additional data suggests that LY 171883 causes membrane hyperpolarization and reduces firing rate of action potentials in neuroblastoma cells in vitro. LY 171883 is an inhibitor of PDE and an activator of PPAR α and PPAR γ.


References

1. Fleisch, J.H., et al. 1985. J. Pharmacol. Exp. Ther. 233: 148-157. PMID: 3981452
2. Aharony, D., et al. 1987. J. Pharmacol. Exp. Ther. 243: 921-926. PMID: 2826761
3. Cannon, J.R. and Eacho, P.I. 1991. Biochem. J. 280: 387-391. PMID: 1747111
4. Li, P.C., et al. 2002. J. Cell. Physiol. 192: 188-199. PMID: 12115725

Physical State :
Solid
Solubility :
Soluble in ethanol (25 mg/ml), DMSO (101 mM), DMF, 0.5M aqueous sodium bicarbonate, and water (15 mg/ml).
Storage :
Store at room temperature
Refractive Index :
n20D 1.57 (Predicted)
IC50 :
Cavia porcellus: IC50 = 1.5 µM; 5-LO: IC50 = 18.9 µM (human); Arachidonate 5-lipoxygenase: IC50 = 18.9 µM (rat); PDE: IC50 = 22.6 µM (human); Cox: IC50 = 44 µM (human)
Ki Data :
CysLT1 Receptor: Ki= 60 nM (human); 3H-LTD4 binding to guinea pig lung membranes: Ki= 0.63 µM
pK Values :
pKa: 5.4 (Predicted), pKb: 1.44 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
KM5780800
PubChem CID :
3969
MDL Number :
MFCD00211057
Beilstein Registry :
4238438
SMILES :
CCCC1=C(C=CC(=C1O)C(=O)C)OCCCCC2=NNN=N2

Download SDS (MSDS)

Certificate of Analysis

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