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.

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.