Dalcetrapib (JTT-705) 是一種具有口服活性的膽固醇酯轉運蛋白 (CETP) 抑制劑，對 rhCETP 和人血漿 CETP 的 IC50 分別為 204.6 nM 和 6 μM。

Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation[1].
Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner[3].

Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits[2].
Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol[1].