GS-5759

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].

Product Specifications

CAS Number

[1346653-91-5]

UNSPSC

12352005

Target

Adrenergic Receptor; Phosphodiesterase (PDE)

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

Field of Research

Inflammation/Immunology

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

Molecular Formula

C47H42N6O8S

Molecular Weight

850.94

References & Citations

[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. |[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.