| Description | A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD). |
| In vitro | A3334 (1-10 μM) efficiently inhibits the adipogenic differentiation of 3T3-L1 preadipocytes via the Wnt/β-eatenin signaling pathway[1]. A3334 (1-10 μM; 24 h) enhances the TOPFlash reporter activity in HEK293-TOP cells[1]. |
| In vivo | A3334 (25 mg/kg; p.o. once daily for 16 weeks) has anti-obesity effects in the HFD mice, and has no effect on mice fed with normal diet[1]. A3334 (25 mg/kg; p.o. once daily for 5 days) significantly reduces fasting glucose and the levels of glucose tolerance (GTT) and insulin tolerance (ITT) in serum in mice[1]. A3334 (25 mg/kg; p.o. once daily for 3 weeks) significantly abolishes hepatosteatosis and the increased levels of alanine transaminase (ALT) and aspartatetransaminase (AST) in mice[1]. Animal Model: Male C57BL/6N mice (6-week-old) are fed on the high fat die (HFD) for 16 weeks[1]Dosage: 25 mg/kg Administration: P.o. daily for 16 weeks Result: Not observed the HFD-induced body weight gain and abdominal obesity. Reduced the level of triglyceride and total cholesterol and increased the level of HDL-cholesterol. Suppressed the increase in adipocyte cell sizes and enhancement of inflammation. |
| Target activity | CXXC5-DVL:63.06 nM (IC50) |
| molecular weight | 307.309 |
| Molecular formula | C17H13N3O3 |
| CAS | 854171-31-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Choi KY, et, al. Compositions and methods for suppressing and/or treating metabolic diseases and/or a clinical condition thereof. WO2020079569. |