LY2484595 (Evacetrapib) |CETP inhibitorCellagen TechnologyPrice from $119.00 to $1,071.00.
Loading...
Loading...
Loading...
Loading...
Cellagen Technology
CETP inhibitor
Dalcetrapib (JTT-705) is a CETP inhibitor of the thioaniline family with a potency of 0.2 uM aimed at raising HDL cholesterol levels. It also inhibits CETP-mediated transfer of CE from HDL to apoB-containing lipoproteins in human plasma at an IC50 of 9 uM. [1] Dalcetrapib is the first molecule that both regulates CETP and demonstrates an anti-atherogenic effect in vivo. [1] It differs from anacetrapib by binding to a different site on CETP, uniquely inducing a conformational change in the CETP molecule which correlates with reduced CETP activity in humans. [3]
Early clinical studies have shown a 26-28% increase in HDL with 600 mg qd dosing. [2] Phase II trials demonstrated that CETP activity was reduced by 50% and HDL levels increased as much as 31%, while LDL levels were unchanged.
Despite halting development in May, 2012, Dalcetrapib remains as a valuable benchmarking tool compound in vitro for modulation of HDL cholesterol levels.
Cellagen Technology
CETP inhibitor
Dalcetrapib (JTT-705) is a CETP inhibitor of the thioaniline family with a potency of 0.2 uM aimed at raising HDL cholesterol levels. It also inhibits CETP-mediated transfer of CE from HDL to apoB-containing lipoproteins in human plasma at an IC50 of 9 uM. [1] Dalcetrapib is the first molecule that both regulates CETP and demonstrates an anti-atherogenic effect in vivo. [1] It differs from anacetrapib by binding to a different site on CETP, uniquely inducing a conformational change in the CETP molecule which correlates with reduced CETP activity in humans. [3]
Early clinical studies have shown a 26-28% increase in HDL with 600 mg qd dosing. [2] Phase II trials demonstrated that CETP activity was reduced by 50% and HDL levels increased as much as 31%, while LDL levels were unchanged.
Despite halting development in May, 2012, Dalcetrapib remains as a valuable benchmarking tool compound in vitro for modulation of HDL cholesterol levels.
