Objective:To investigate the effect of BVT.2733 on insulin resistance(IR) and inflammation in diet-induced obesity(DIO)mice. Methods:Male mice were divided into normal mice and model mice after fed with normal diet and high-fat diet for 20 weeks,respectively. The model mice were subdivided into BVT.2733 mice administrated with BVT.2733 and obesity mice with placebo for 2 weeks. Indexes related with metabolism and inflammation were measured. Results:Compared with normal mice,adipocytes were significantly enlarged in obesity mice,and body weight also increased. Similarly,blood glucose,serum insulin and TNF-α,the expression of TLR4 mRNA in adipose tissue were all increased. After administration of BVT.2733,adipocytes were diminished; body weight,blood glucose,serum insulin,and the expression of TLR4 mRNA in adipose tissue were all decreased. But there was no significant change in serum TNF-α. Conclusion:BVT.2733 can improve IR and decrease the expression of TLR4 mRNA in adipose tissue,but have little effect on serum TNF-α in DIO mice.