Aim To evaluate the effects of Methyl 3β-hydroxy-5α, 6α-epoxycholanate (MHEC) and T-0901317 on the expression of ATP-binding cassette transporter A1 (ABCA1), liver X receptors (LXR)αand LXR β in THP-1 cells. Methods THP-1 cells were cultured and treated with LXRs agonists MHEC and T-0901317 respectively. The mRNA expressions of ABCA1, LXRα and LXRβ were detected by reverse transcription-polymerase chain reaction (RT-PCR). Immunohistochemical method was used to assess the expression of ATP-binding cassette transporter A1 protein in the cells. Results Both of the two LXR agonists' treatment significantly increased ABCA1 mRNA and LXRα mRNA in a time and dose-dependent fashion in THP-1 cells. The expression of ATP-binding cassette transporter A1 protein also increased in the treated cells. While the LXRβ expression in T-0901317 group was stronger than in MHEC group. Conclusions Both MHEC and T-0901317 can up-induce the expressions of ATP-binding cassette transporter A1 and LXRα in THP-1 cells, and MHEC is more likely to be a selective agonist to LXRα.