DL5050 is a selective agonist for the human constitutive androstane receptor (hCAR). This compound demonstrates superior affinity and selectivity for hCAR by inducing expression of CYP2B6 (the target of hCAR) at the mRNA and protein levels, rather than CYP3A4 (the target of the human pregnane X receptor, hPXR). As a selective hCAR agonist, DL5050 not only serves as a crucial tool molecule for studying hCAR's biological function but also holds potential as a lead compound for the development of therapeutic applications targeting hCAR.