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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)