| Identification | Back Directory | [Name]
Fargesone A | [CAS]
116424-69-2 | [Synonyms]
Fargesone A
(2S,3R,3aR,7S,7aS)-2-(1,3-benzodioxol-5-yl)-3a,4-dimethoxy-3-methyl-7-prop-2-enyl-2,3,7,7a-tetrahydro-1-benzofuran-6-one
6(2H)-Benzofuranone, 2-(1,3-benzodioxol-5-yl)-3,3a,7,7a-tetrahydro-3a,4-dimethoxy-3-methyl-7-(2-propen-1-yl)-, (2R,3S,3aS,7S,7aR)-
[2R-(2alpha,3beta,3abeta,7alpha,7abeta)]-2-(1,3-Benzodioxol-5-yl)-3,3a,7,7a-tetrahydro-3a,4-dimethoxy-3-methyl-7-(2-propenyl)-6(2H)-benzofuranone | [Molecular Formula]
C21H24O6 | [MDL Number]
MFCD26406196 | [MOL File]
116424-69-2.mol | [Molecular Weight]
372.41 |
| Hazard Information | Back Directory | [Uses]
Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity[1]. | [Definition]
ChEBI: Fargesone A is a member of benzodioxoles. | [in vivo]
Fargesone A (3 and 30 mg/kg; i.p.; daily for 7 days) significantly ameliorates pathological features in bile duct ligation (BDL)-induced chronic liver fibrosis mouse model[1].
Pharmacokinetics parameters of Fargesone A in mice
| t1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (ng/mL*h) | AUC0-inf (ng/mL*h) | MRT0-inf (h) | F (%) | | i.v. (5 mpk) | 0.68±0.1 | - | 941±57 | 469±13 | 471±14 | 0.43±0.13 | - | | p.o. (10 mpk) | 0.33±0.04 | 0.25±0.00 | 104±16 | 101±32 | 102±32 | 0.58±0.07 | 10.8±3.2 |
| Animal Model: | C57BL/6 mice, bile duct ligation (BDL)-induced chronic liver fibrosis mouse model[1] | | Dosage: | 3 and 30 mg/kg | | Administration: | IP, once daily for 7 days | | Result: | Resulted in a lower level of inflammatory infiltrates and a smaller amount of collagen deposition compared to the vehicle group. Reversed BDL-induced sharp increase in total bilirubin level in the serum. Significantly decreased liver mRNA expression of the inflammatory biomarkers interleukin (IL)-6, IL-1β, inducible nitric oxide synthase (iNOS), and prostaglandin-endoperoxide synthase 2 (COX2). |
| Animal Model: | C57BL6/J mice[1] | | Dosage: | 5 or 10 mg/kg | | Administration: | IV or PO (Pharmacokinetics Analysis) | | Result: | Showed acceptable PK profiles in general. |
| [References]
[1] Guo F, et al. Biomimetic Total Synthesis and the Biological Evaluation of Natural Product (-)-Fargesone A as a Novel FXR Agonist. JACS Au. 2022 Dec 7;2(12):2830-2838. DOI:10.1021/jacsau.2c00600 |
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