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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2018.6
- 수록면
- 61 - 65 (5page)
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KPLA-012, a benzopyranyl 1,2,3-triazole compound, is considered a potent HIF-1α inhibitor based on the chemical library screening, and is known to exhibit anti-angiogenetic and anti-tumor progressive effects. The aim of this study was to investigate the pharmacokinetic properties of KPLA-012 in ICR mice and to investigate in vitro characteristics including the intestinal absorption, distribution, metabolism, and excretion of KPLA-012. The oral bioavailability of KPLA-012 was 33.3% in mice. The pharmacokinetics of KPLA-012 changed in a metabolism-dependent manner, which was evident by the low recovery of parent KPLA-012 from urine and feces and metabolic instability in the liver microsomes. However, KPLA-012 exhibited moderate permeability in Caco-2 cells (3.1 × 10
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