| Identification | Back Directory | [Name]
Spiro[[1]benzoxepino[3,2-b]pyridine-11(10H),1'-cyclopropane]-7-carboxylic acid, 2-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]- | [CAS]
2181834-03-5 | [Synonyms]
Spiro[[1]benzoxepino[3,2-b]pyridine-11(10H),1'-cyclopropane]-7-carboxylic acid, 2-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]- | [Molecular Formula]
C29H22Cl2N2O5 | [MOL File]
2181834-03-5.mol | [Molecular Weight]
549.4 |
| Chemical Properties | Back Directory | [Boiling point ]
744.9±60.0 °C(Predicted) | [density ]
1.55±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
4.01±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis[1]. | [in vivo]
HEC96719 (0.5, 1.5 and 5 mg/kg; oral administration, once daily for 14 days) shows in vivo efficacy for the activation of FXR by measuring the increasing level of fibroblast growth factor 15 (FGF15)[1].
HEC96719 (5 mg/kg; oral administration, once) increases the level of liver bile salt export pump (BSEP) and ileum FGF15[1].
HEC96719 (0.1, 0.3 and 1 mg/kg; oral administration, once daily for 6 weeks) significantly improves NASH symptoms[1].
HEC96719 (0.1, 0.3 and 1 mg/kg; oral administration, once daily for 4 weeks) shows efficacy for improving liver fibrosis and has better effects than obeticholic acid (OCA)[1]. | Animal Model: | Male ob/ob nonalcoholic steatohepatitis (NASH) mouse models[1] | | Dosage: | 0.1, 0.3 and 1 mg/kg | | Administration: | Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 6 weeks | | Result: | Decreased levels of serum alanine aminotransferase (ALT) and liver triglyceride (TG), dose-dependently increased NASH activity and reduced NASH activity score.
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| Animal Model: | Male C57BL/6 liver fibrosis mouse models[1] | | Dosage: | 0.1, 0.3 and 1 mg/kg | | Administration: | Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 4 weeks | | Result: | Decreased levels of serum ALT and TBIL, and reduced fibrosis area.
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| [References]
[1] Cao S, et al. Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis. Eur J Med Chem. 2022 Feb 15;230:114089. DOI:10.1016/j.ejmech.2021.114089 |
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| Company Name: |
Biorbyt Ltd.
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| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
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