1346653-91-5
Chemical Structure
GS-5759
- CAS No.: 1346653-91-5
- Formula:C47H42N6O8S
- Molecular Weight:850.94
IUPAC Name: (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
InChIKey: HJBZAZITZDSWKD-RWYGWLOXSA-N
SMILES: O=C(C1=C(NC2=CC=CC(OC)=C2)C3=CC(S(=O)(C4=CC=CC(C(NC5=CC=C(C#CCCCNC[C@@H](C6=CC=C(O)C7=C6C=CC(N7)=O)O)C=C5)=O)=C4)=O)=CC(C)=C3N=C1)N
Biological Activity: GS-5759 is both a β₂-adrenergic receptor agonist and a PDE4 inhibitor. GS-5759 increases intracellular cAMP levels by activating the β₂ receptor, promoting bronchial dilation. GS-5759 inhibits PDE4 activity, reduces cAMP degradation, and enhances anti-inflammatory effects. GS-5759 exhibits potent bronchial dilation and anti-inflammatory capabilities in animal models. GS-5759 can be used for research on respiratory diseases such as chronic obstructive pulmonary disease (COPD)[1][2].
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GS-5759 | 99.21% | GS-5759 is both a β₂-adrenergic receptor agonist and a PDE4 inhibitor. GS-5759 increases intracellular cAMP levels by activating the β₂ receptor, promoting bronchial dilation. GS-5759 inhibits PDE4 activity, reduces cAMP degradation, and enhances anti-inflammatory effects. GS-5759 exhibits potent bronchial dilation and anti-inflammatory capabilities in animal models. GS-5759 can be used for research on respiratory diseases such as chronic obstructive pulmonary disease (COPD). | ||||||||||||||||||||
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- [1]. Joshi T, et al. GS-5759, a Bifunctional β2-Adrenoceptor Agonist and Phosphodiesterase 4 Inhibitor for Chronic Obstructive Pulmonary Disease with a Unique Mode of Action: Effects on Gene Expression in Human Airway Epithelial Cells. J Pharmacol Exp Ther. 2017 Feb;360(2):324-340. [Content Brief]
- [2]. Salmon M, et al. The in vivo efficacy and side effect pharmacology of GS-5759, a novel bifunctional phosphodiesterase 4 inhibitor and long-acting β 2-adrenoceptor agonist in preclinical animal species. Pharmacol Res Perspect. 2014 Aug;2(4):e00046. [Content Brief]
Keywords