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JTT-705 (Dalcetrapib) | CETP inhibitor

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Price:
$159.00
Catalog #:
C5705-2s
Quantity:


Product Description

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.

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