A3051是一种有效的和具有口服活性的CXXC5-DVL的抑制剂，IC50值为63.06nM。A3334可用于研究高脂肪饮食(HFD)和蛋氨酸-胆碱缺乏饮食(MCD)诱导的疾病，例如肥胖，糖尿病和NASH。详细信息请参考专利文献WO2020079569。
A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH[1].
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].
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]
[1]. Choi KY, et, al. Compositions and methods for suppressing and/or treating metabolic diseases and/or a clinical condition thereof. WO2020079569.
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