Species-dependent affinity of PepT1 for valacyclovir
| Animal Species | VACV Km (mM) | Experimental Conditionsa | Reference |
|---|---|---|---|
| Human | 0.3 | Caco-2, pH 7.4, HPLC-UV | Han et al., 1998 |
| Human | 5.9 | cRNA-injected XLO, pH 5.5, [3H]label-LSC | Balimane et al., 1998 |
| Human | 1.6 | cDNA-transfected CHO, pH 7.5, [3H]label-LSC | Guo et al., 1999 |
| Human | 2.2-7.4 | cDNA-transfected CHO, pH 7.9–5.5, [3H]label-LSC | Balimane and Sinko, 2000 |
| Human | 1.6 | Caco-2, pH 6.0, [3H]label-LSC | Bhardwaj et al., 2005 |
| Human | 3.8-5.0 | cDNA-transfected MDCK, pH 6.0, [3H]label-LSC | Bhardwaj et al., 2005 |
| Rat | 1.2b | Single-pass jejunal perfusion, pH 6.5, HPLC-UV | Sinko and Balimane, 1998 |
| Mouse | 10.2 | Single pass jejunal perfusion, pH 6.5, HPLC-FL | Yang and Smith, 2013a |
↵a Caco-2 refers to human epithelial colorectal adenocarcinoma cells.
CHO, Chinese hamster ovary cells; FL, fluorescent detection; LSC, liquid scintillation counter; MDCK, Mardin-Darby canine kidney epithelial cells; UV, ultraviolet; VACV, [3H]label to the radioisotope of valacyclovir; XLO, Xenopus laevis oocytes.
↵b Intrinsic Km calculated using “estimated” concentrations at the membrane wall.