Fargesone A
Fargesone A Basic information
- Product Name:
- Fargesone A
- Synonyms:
-
- Fargesone A
- [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
- 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)-
- (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
- CAS:
- 116424-69-2
- MF:
- C21H24O6
- MW:
- 372.41
- Mol File:
- 116424-69-2.mol
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Fargesone A Chemical Properties
- Boiling point:
- 508.0±50.0 °C(Predicted)
- Density
- 1.25±0.1 g/cm3(Predicted)
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Fargesone A Usage And Synthesis
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
Fargesone ASupplier
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