Drug intelligence / Profile preview

fargesin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraarticular, Oral
01

Overview

Fargesin is a naturally occurring tetrahydrofurofuranoid lignan isolated from various traditional medicinal plants, including *Magnolia fargesii*, *Magnolia biondii*, *Zanthoxylum armatum*, and *Chrysanthemum indicum*. It exhibits a wide range of pharmacological activities, including anti-inflammatory, anti-allergic, cardioprotective, anti-cancer, and neuroprotective effects. Preclinical studies have demonstrated that fargesin acts as a potential beta-1 adrenergic receptor (ADRB1) antagonist, protecting against myocardial ischemia/reperfusion injury, and inhibits the ORAI1 calcium channel to suppress T-cell activation and mast cell degranulation. Additionally, fargesin has been shown to target pyruvate kinase PKM2 to inhibit aerobic glycolysis in non-small cell lung cancer, suppress BRD4 expression to alleviate intervertebral disc degeneration, and activate the aryl hydrocarbon receptor (AhR) to protect against lung injury. It is primarily investigated as a research reagent and natural bioactive compound.

Other names
(+)-fargesin(±)-fargesin1,3-benzodioxole, 5-[(1R,3aS,4S,6aS)-4-(3,4-dimethoxyphenyl)tetrahydro-1H,3H-furo[3,4-c]furan-1-yl]-, rel-5-[(3S,3aR,6R,6aR)-6-(3,4-dimethoxyphenyl)-1,3,3a,4,6,6a-hexahydrofuro[3,4-c]furan-3-yl]-1,3-benzodioxoleFarFGSrel-5-[(1R,3aS,4S,6aS)-4-(3,4-dimethoxyphenyl)tetrahydro-1H,3H-furo[3,4-c]furan-1-yl]-1,3-benzodioxole
02

Targets

NF-κBAHR (Aryl hydrocarbon receptor)ADRB1 (β1)ORAI1 (Calcium release–activated calcium channel protein 1)

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