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Table 4 Summary of microsomal half-life and clearance in vitro of SJ733 and SJ311

From: Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones

Species Parameter (-)-SJ733 (+)-SJ733 (−)-SJ311 (+)-SJ311
Mouse t1/2 (h) 0.8 ± 0.1 0.7 ± 0.1  > 4  > 4
CLint (µl/min/mg protein) 32.1 ± 2.1 35.4 ± 2.1  < 7  < 7
Rat t1/2 (h)  > 4  > 4  > 4  > 4
CLint (µl/min/mg protein)  < 7  < 7  < 7  < 7
Dog t1/2 (h) 2.2 ± 0.4  > 4  > 4  > 4
CLint (µl/min/mg protein) 10.9 ± 1.5  < 7  < 7  < 7
Human t1/2 (h) 0.4 ± 0.1 0.5 ± 0.1  > 4  > 4
CLint (µl/min/mg protein) 61.7 ± 13.2 45.5 ± 4.0  < 7  < 7
  1. Compounds with a calculated half-life longer than 4 h were all reported as having a half-life of > 4 h, and a clearance value < 7 µl/min/mg protein. Compounds were tested at a concentration of 0.8 µM. Data were presented as mean ± SD (n = 3)
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