Table 1.
In Vitro and Pharmacokinetic Activity of PSZ and initial Des-triazole PSZ Analogue.
| Cmpd | IC50 (μM)a | Ptch-CKO GI50 (μM)b |
CYP3A4 IC50 (μM)c |
P-gp Substratec |
T1/2 (min)c |
Clint (μL/min/mg)c |
|---|---|---|---|---|---|---|
| PSZ | 0.50 ± 0.1 | 1.5 ± 0.3 | 0.15 | Yes | 108 | 21.5 |
| 1 | 0.19 ± 0.03 | 0.61 ± 0.12 | >20 | No | 61.8 | 37.4 |
a
IC50 values from ASZ cells represent the Mean ± SEM of at least two separate experiments performed in triplicate following a 48 hr incubation.
b
Values represent the Mean ± SEM of at least two separate experiments performed in triplicate.
c
PK data generated by Pharmaron or Cyprotex as a CRO service via their standard protocols.