Table S1.
Pharmacokinetic data for PDZ1i
| PK parameters | Mean ± SD | CV, % |
| I.v. study | ||
| Body weight | 25.1 ± 0.173 g | 0.690 |
| I.v. time, h | ||
| 0 | 35,033 ± 9,424 ng/mL | 26.9 |
| 0.250 | 29,533 ± 7,387 ng/mL | 25.0 |
| 1.00 | 17,733 ± 3,630 ng/mL | 20.5 |
| 2.00 | 11,600 ± 985 ng/mL | 8.49 |
| 6.00 | 6,113 ± 531 ng/mL | 8.68 |
| 12.0 | 3,360 ± 927 ng/mL | 27.6 |
| 24.0 | 541 ± 79.6 ng/mL | 14.7 |
| C0 | 35,033 ± 9,424 ng/mL | 26.9 |
| T1/2* | 5.06 ± 0.285 h | 5.64 |
| AUC0-last | 120,000 ± 17,692 ng·h−1⋅mL−1 | 14.7 |
| AUC0-inf | 124,000 ± 17,349 ng·h−1⋅mL−1 | 14.0 |
| I.p. study | ||
| Body weight | 24.5 ± 0.252 g | 1.03 |
| I.p. time, h | ||
| 0 | ND | ND |
| 0.250 | 98,233 ± 10,289 ng/mL | 10.5 |
| 1.00 | 69,233 ± 9,757 ng/mL | 14.1 |
| 2.00 | 58,967 ± 7,257 ng/mL | 12.3 |
| 6.00 | 54,600 ± 6,351 ng/mL | 11.6 |
| 12.0 | 42,833 ± 7,129 ng/mL | 16.6 |
| 24.0 | 15,133 ± 2,754 ng/mL | 18.2 |
| Cmax | 98,233 ± 10,289 ng/mL | 10.5 |
| Tmax | 0.250 ± 0.000 h | 0.00 |
| T1/2* | 9.42 ± 0.585 h | 6.22 |
| AUC0-last | 974,667 ± 127,602 ng·h−1⋅mL−1 | 13.1 |
| AUC0-inf | 1,183,333 ± 180,093 ng·h−1⋅mL−1 | 15.2 |
| Bioavailability, i.p./i.v. | 81.2 ± 10.6% |
Plasma concentration (ng/mL) in mice (n = 3) after i.v. (3 mg/kg) and i.p. (30 mg/kg) administration, measured at time points reported under I.v. time and I.p. time, respectively. BALB/c mice (n = 3 per group) were injected with 3 mg/kg and 30 mg/kg PDZ1i i.v. or i.p., respectively, and the average concentration of intact compound in plasma was determined via HPLC at the indicated time points. AUC0-inf, area under the curve of plasma concentration versus time calculated between time 0 and an extrapolated infinite time point; AUC0-last, area under the curve of plasma concentration versus time calculated between time 0 and last measured time point; C0 = concentration at time 0; Cmax = maximal concentration observed; CV, coefficient of variation; ND, not determined; SD, standard deviation.
Three time points were used for T1/2.