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LY171883

Cayman Chemical Item Number 70710

(CAS 88107-10-2)

LY171883 (CAS 88107-10-2)

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Description

LY171883 is a selective, potent, orally active antagonist of the leukotriene D4 receptor.1 Dissociation constants (KB) for LY171883 on guinea pig ileum and parenchyma are 0.07 and 0.34 µM, respectively.1 LY171883 is an inhibitor of phosphodiesterase obtained from human polymorphonuclear leukocytes (IC50 of 22.6 µM) and various guinea pig tissues (IC50s range from 6.9-209 µM).1 At a concentration of 50-100 µM, LY171883 binds to the PPARγ nuclear receptor, inducing adipogenesis in cultured NIH3T3 fibroblasts.2,3

1 Fleisch, J.H., Rinkema, L.E., Haisch, K.D., et al. LY171883, 1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]ethanone, an orally active leukotriene D4 antagonist. J Pharmacol Exp Ther 233 148-157 (1985).

2 Sala, A., Rossoni, G., Buccellati, C., et al. Formation of sulphidopeptide-leukotrienes by cell-cell interaction causes coronary vasoconstriction in isolated, cell-perfused heart of rabbit. Br J Pharmacol 110 1206-1212 (1993).

3 Tontonoz, P., Hu, E., and Spiegelman, B.M. Stimulation of adipogenesis in fibroblasts by PPARγ2, a lipid-activated transcription factor. Cell 79 1147-1156 (1994).

Formal Name 1-​[2-​hydroxy-​3-​propyl-​4-​[4-​(1H-​tetrazol-​5-​yl)butoxy]phenyl]-​ethanone
CAS Number 88107-10-2
Molecular Formula C16H22N4O3
Formula Weight 318.4
Formulation A crystalline solid
Purity >98%
λmax 218, 284 nm
Stability 2 years
Storage Room temperature
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CCCc1c(OCCCCc2nnn[nH]​2)​ccc(C(=O)​C)​c1O

Background Reading

Fleisch, J.H., Rinkema, L.E., Haisch, K.D., et al. LY171883, 1-[2-hydroxy-3-propyl-4-[4-(1H-tetrazol-5-yl)butoxy]phenyl]ethanone, an orally active leukotriene D4 antagonist. J Pharmacol Exp Ther 233 148-157 (1985).

Tontonoz, P., Hu, E., and Spiegelman, B.M. Stimulation of adipogenesis in fibroblasts by PPARγ2, a lipid-activated transcription factor. Cell 79 1147-1156 (1994).

Sala, A., Rossoni, G., Buccellati, C., et al. Formation of sulphidopeptide-leukotrienes by cell-cell interaction causes coronary vasoconstriction in isolated, cell-perfused heart of rabbit. Br J Pharmacol 110 1206-1212 (1993).

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