Inhibition parameters of NSAIDs and NSAIDs-Glu for uptake of MTX via MRP2
| NSAID | IC50 (μM) | R/S Ratio | Glucuronide/Aglycone Ratio | Hill Slope | |||
|---|---|---|---|---|---|---|---|
| Aglycone | Glucuronide | Aglycone | Glucuronide | Aglycone | Glucuronide | ||
| Diclofenac | 139 (128‒151)a | 18.6 (15.7‒21.9) | —b | — | 0.13 | 2.78 | 1.26 |
| R-ibuprofen | 303 (252‒365) | 208 (189‒229) | 2.19 | 2.57 | 0.69 | 1.52 | 1.87 |
| S-ibuprofen | 139 (113‒171) | 80.9 (74.2‒88.2) | 0.58 | 1.24 | 1.93 | ||
| R-flurbiprofen | 133 (112‒158) | 29.5 (23.9‒36.3) | 2.28 | 1.37 | 0.22 | 2.17 | 1.04 |
| S-flurbiprofen | 58.4 (50.4‒67.6) | 21.5 (19.4‒23.8) | 0.37 | 1.43 | 1.39 | ||
| R-naproxen | 510 (465‒559) | 771 (727‒817) | 71.7 | 1.62 | 1.51 | 3.28 | 3.75 |
| S-naproxen | 7.11 (5.21‒9.70) | 475 (449‒504) | 66.8 | 0.46 | 1.79 | ||