GS-5759 | PDE4 inhibitor, β2-adrenoceptor agonist

Chemical Structure : GS-5759

GS-5759 (GS 5759, GS5759)

Catalog No.: PC-60211Not For Human Use, Lab Use Only.

GS-5759 is a novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).

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Biological Activity

GS-5759 is a novel bifunctional PDE4 inhibitor (IC50=5 nM) and long acting β2-adrenoceptor agonist (EC50=8 nM).
GS-5759 inhibits LPS-induced TNFα production in human PBMC (IC50=0.3 nM) and in human neutrophils fMLP-induced super oxide anion production (IC50=3 nM).
GS-5759 also is a potent inhibitor of profibrotic and proinflammatory mediator release from human lung fibroblasts.

Physicochemical Properties

M.Wt	850.95
Formula	C47H42N6O8S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-6-[(3-{[4-(5-{[2-Hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}pent-1-yn-1-yl)phenyl]carbamoyl}phenyl)sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methylquinoline-3-carboxamide

References

1. Tannheimer SL, et al. J Pharmacol Exp Ther. 2014 Apr;349(1):85-93.

2. Joshi T, et al. J Pharmacol Exp Ther. 2017 Feb;360(2):324-340.

GS-5759 (GS 5759, GS5759)

Biological Activity

Physicochemical Properties

References

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