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. 2021 May 25;12(6):969–975. doi: 10.1021/acsmedchemlett.1c00082

Table 3. In Vitro and In Vivo Characterization of 2b, 2d, and 3.

graphic file with name ml1c00082_0007.jpg

  2b 2d 3
CYPa IC50 (μM)      
3A4/2D6 > 40 > 40 > 40 > 40 > 40 > 40
2C9/2C19 > 40 > 40 > 40 > 40 > 40 > 40
hERG patch clamp: % Inh @ 30 μM 24 19 36
Na+ patch clamp: % Inh @ 30 μM, 4 Hz 2.5 13 65
protein binding %free:      
human/cyno/dog 50/65/78 59/49/51  
rat/mouse 53/51 53/47  
mouse PK data (IV: 2 mg/kg; PO: 10 mg/kg)      
AUC0–24h (μM·h)/F (%) 2.0/38 5.4/93  
Cl (mL/min/kg)/T1/2 (h) 70/2.6 63/4.1  
a

CYP = cytochrome P450.