Table 4. Rat PKa on Analogs Meeting In Vitro Criteria.
Cmaxb (μM) | %F | Cl mL min–1 kg–1 | Vd L/kg | frac. abs.c | |
---|---|---|---|---|---|
1 | 0.32 | 20% | 6.9 | 0.95 | 22% |
14b | 1.4 | 100% | 11 | 3.9 | 100% |
14c | 1.6 | 94% | 7.0 | 1.3 | 100% |
15a | 0.57 | 35% | 10 | 1.6 | 41% |
iv 1 mpk (n = 3), po 4 mpk in 0.5% methylcellulose (n = 3).
po dosing.
Fraction absorbed estimated from bioavailability (%F), Cl, and hepatic blood liver flow (Qh) = 70 mL min–1 kg–1.13