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. AUC_0-inf, area under the curve of plasma concentration versus time calculated between time 0 and an extrapolated infinite time point; AUC_0-last, area under the curve of plasma concentration versus time calculated between time 0 and last measured time point; C₀ = concentration at time 0; C_max = maximal concentration observed; CV, coefficient of variation; ND, not determined; SD, standard deviation.

^*Three time points were used for T_1/2.