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:
| Chemical Formula: | C23H35NO2S | |
| CAS #: | 211513-37-0 | |
| Molecular Weight: | 389.59 | |
| Purity: | > 98% | |
| Appearance: | Light Yellow | |
| Chemical Name: | S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | JTT-705, JTT705, Dalcetrapib, RO4607381 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Shinkai, H., Cholesteryl ester transfer-protein modulator and inhibitors and their potential for the treatment of cardiovascular diseases. Vascular Health and Risk Management, 2012, 8, 323-331. Pubmed ID: 22661899 |
| 2. | Goldberg et al., Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib. Drug Design, Development, and Therapy, 2012, 6, 251-259. Pubmed ID: 23055695 |
| 3. | Durrington, Br. J. Cardiol. 2012, 19(3), 126-133 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
