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. 2020 Mar 10;11(4):550–557. doi: 10.1021/acsmedchemlett.0c00010

Table 2. Pharmacokinetic Parameters on Selected Compounds.

Cmpd AlogP98 Rat in vivo Clint (mL/min/kg), Vdu (L/kg), MRT (h) Predicted Human QD Dosed
1 4.4 >Qhepc, 180, 0.7a >10 g
3 5.3 6000, 1100, 4.3a 16 mg
9 4.7 4500, 2200, 5.0b 280 mg
11 3.8 1600, 420, 4.8a 6 mg
12 3.1 590, 99, 3.2a 26 mg
a

Protocol Rat Cassette: route IV; Dose 0.05 mg/kg; Dose Vol 1 mL/kg; formulation DMSO/PEG400/H2O-20/60/20; Fasted.

b

Protocol Rat 2 × 2: route IV; Dose 0.5 mg/kg; Dose Vol 1 mL/kg; formulation DMSO/PEG400/H2O-20/60/20; route PO; Dose 1 mg/kg; Dose Vol 2 mL/kg; formulation DMSO/PEG400/H2O-20/60/20.

c

Reported assay data is the geometric mean of n = 2 or greater.

d

Based on rat allometry.