Skip to main content
. 2021 May 13;12(6):1005–1010. doi: 10.1021/acsmedchemlett.1c00160

Table 3. Pharmacokinetics of Selected Compoundsa.

    dose
         
species compd iv po CL Vd t1/2 DNAUCpo F
ratb 2 0.5e 10 91.2 4.42 0.72 37.7 3.6
  19 0.5e   45.9 2.1 0.62    
  20 2 5 1.88 0.81 5.20 1293 14.5
  21 0.5 8.6 3.48 0.97 3.89 6651 133
          
mousec 21 1 3 1.44 1.34 10.9 5831 37.1
          
dogd 21 1 2 3.15 2.12   2937 52.2
a

Dose: mg/kg; CL: mL/min/kg; Vd: L/kg; DNAUCpo: (ng*h/mL)/(mg/kg); t1/2: hour; F: %, n ≥ 2. For compound 21: rat iv formulation: 1.00 mg/mL in DMSO:PEG400:Water (10:45:45), po formulation: 2.00 mg/mL in 1% HPMC/water(1:1). Mouse iv formulation: 1 mg/mL in 20%HP-beta-CD in saline, pH = 8, po formulation: 3 mg/mL in 0.5% HPMC. Dog iv Formulation: 0.25 mg/mL in 5% DMSO:20% HP-Beta-CD in saline, po formulation: 0.5 mg/mL in 5% DMSO:6% HP-β-CD in saline, pH 10.3.

b

Sprague–Dawley rats, fasted.

c

Male C57 mouse, fasted.

d

Male beagle dogs, fasted.

e

iv: cassette dosing.