Abstract: OBJECTIVE To introduce approaches and techonologies for validating the stable expression of drug transporters in vitro, and provide suggestions for application in cellular models. METHODS Review related literatures about the recent research progress on stably expressing transporters in transfected cells. RESULTS Real-time polymerase chain reaction and Western blot were classical methods respectively for detecting the expression of messenager ribonucleic acid (mRNA) and protein. CONCLUSION The combination of real time-PCR,Western blot with fluorescence detection techonology have promising applications in verifying the stable expression of transporter in different levels including transcription, protein expression and functional activity.