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. 2020 Mar 6;63(7):3577–3595. doi: 10.1021/acs.jmedchem.9b02036

Table 6. In Vitro Stability and in Vivo Pharmacokinetic Properties of Selected Compounds in Mice.

          iv dosing (5 mg/kg)
po dosing (10 mg/kg)
 
  cAMP pEC50a aq. sol. (μM)a log D7.4a MLM (%)b t1/2 (min) Vd (mL/kg) CLtotal (mL/min/kg) t1/2 (min) tmax (min) cmax (ng/mL) AUCinf (ng.min/mL) F (%)
1 6.28 190 2.05 52 62.2 759 8.45 89.7 15 7470 865 000 73
16 6.89 5 3.19 1 22.3 629 19.6 60.8 30 5740 423 000 88
35 5.92 199 2.64 23                
47 6.60 1 3.39 2                
51 6.72 1 2.59 12                
57 6.84 33 4.25 1 11.4 1150 70.3 63.5 30 561 33 800 36
62 6.60 5 3.73 1                
63 6.79 9 >4.3 41 37.8 1110 20.3 51.8 15 3800 325 000 66
a

Most data are replicated from Tables 1 and 35 (for SEM and Emax, see these tables).

b

Remaining after 40 min incubation with MLMs.