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    Dalcetrapib (JTT-705, RO4607381)
    Dalcetrapib (JTT-705, RO4607381)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0914
    CAS #: 211513-37-0Purity ≥98%

    Description: Dalcetrapib (aslo known as JTT-705 and RO4607381) is a novel, potent and selective rhCETP (Cholesteryl ester transfer protein) inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Dalcetrapib was aimed at raising the blood levels of 'good cholesterol' (cholesterol carried in HDL particles, aka HDL-C). Prevailing observations indicate that high HDL levels correlate with better overall cardiovascular health, though it remains unclear whether raising HDL levels consequently leads to an increase in cardiovascular health. Cholesteryl ester transfer protein, also called plasma lipid transfer protein, is a plasma protein that facilitates the transport of cholesteryl esters and triglycerides between the lipoproteins.

    References: J Lipid Res. 2010 Dec;51(12):3443-54; J Med Chem. 2000 Sep 21;43(19):3566-72.

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    • 香港大学
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    Molecular Weight (MW)389.59
    FormulaC23H35NO2S
    CAS No.211513-37-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (200.2 mM)
    Water: <1 mg/mL
    Ethanol: 78 mg/mL (200.2 mM)
    Solubility (In vivo)0.5% methylcellulose: 30 mg/mL
    SynonymsDalcetrapib; JTT-705; RO-4607381; RO4607381; RO 4607381; JTT705; JTT 705


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    In Vitro

    In vitro activity: Dalcetrapib modulates CETP activity. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-β-HDL formation in human plasma is unchanged by Dalcetrapib ≤3 µM and increased at 10 µM. Dalcetrapib statistically and significantly increases pre-β-HDL formation. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner.


    Kinase Assay: The inhibitory potency (IC50) of Dalcetrapib to decrease CE transfer from HDL to LDL by rhCETP and C13S CETP is measured using a scintillation proximity assay kit. Briefly, [3H]CE-labeled HDL donor particles are incubated in the presence of purified CETP proteins (final concentration 0.5 µg/mL) and biotinylated LDL acceptor particles for 3 hours at 37 °C. Subsequently, streptavidin-coupled polyvinyltoluene beads containing liquid scintillation cocktail binding selectively to biotinylated LDL are added, and the amount of [3H]CE molecules transferred to LDL is measured by β counting. 


    Cell Assay: The HepG2 cells are seeded in 6-well plates and cultured to 70–80% confluence. After being washed with PBS, the cells are incubated with growth medium and a different concentration (0 μM–30 μM) of chemical inhibitor Dalcetrapib and dissolved in 2% DMSO for 24 hours. Total RNA is used for RT-PCR.

    In VivoTreatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [3H]cholesterol-labeled autologous macrophages Dalcetrapib significantly increases fecal elimination of both [3H]neutral sterols and [3H]bile acids. Dalcetrapib increases plasma HDL-[3H]cholesterol. Dalcetrapib has 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits. Treatment with Dalcetrapib markedly increases serum levels of HDL-C. The ratio of HDL2-C to HDL3-C is significantly higher in Dalcetrapib–treated rabbits than in control rabbits at 5 and 7 months, indicating that the inhibition of CETP activity by Dalcetrapib changes the distribution of HDL subfractions and preferentially increases HDL2-C levels. Dalcetrapib treatment increases serum paraoxonase activity and HDL-associated platelet-activating factor acetylhydrolase activity, but decreases the plasma lysophosphatidylcholine concentration.
    Animal modelSyrian hamsters
    Formulation & DosageDissolved in  0.5% methylcellulose; 100 mg/kg; Oral gavage  
    References

    J Lipid Res. 2010 Dec;51(12):3443-54; J Med Chem. 2000 Sep 21;43(19):3566-72.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Dalcetrapib (JTT-705, RO4607381)

    [3H]cholesteryl ester-labeled HDL3 was incubated with unlabeled HDL2 and recombinant human cholesteryl ester transfer protein [(rh)CETP] in the presence of: (A) dalcetrapib, 0.01 µM to 10 µM (n = 3); (B) dalcetrapib, 1 µM and 10 µM, torcetrapib and anacetrapib. J Lipid Res.2010 Dec;51(12):3443-54.

    Dalcetrapib (JTT-705, RO4607381)

    A: Competition of [14C]torcetrapib (0.25 μM) and unlabeled CETP inhibitors for binding to rhCETP. B: Displacement of [14C]dalcetrapib in the presence of reducing agent tris(2-carboxyethyl)phosphine (TCEP) by CETP inhibitors after preincubation. J Lipid Res. 2010 Dec;51(12):3443-54.

    Dalcetrapib (JTT-705, RO4607381)

    Schematic depicting action of CETP and proposed effects of dalcetrapib and torcetrapib. J Lipid Res.2010 Dec;51(12):3443-54.


     

    Dalcetrapib (JTT-705, RO4607381)

    A: Human plasma with an endogenous CETP level of 1.25 μg/ml was incubated for 21 h with and without test compounds, dalcetrapib, torcetrapib, and anacetrapib (0.1, 1, 3, and 10 µM). J Lipid Res.2010 Dec;51(12):3443-54.

     

    Dalcetrapib (JTT-705, RO4607381)

    Comparison of the effect of dalcetrapib, torcetrapib, and anacetrapib on HDL-C·AUC and radioactivity of fecal total sterols as a percentage of injected radioactivity in the hamster macrophage reverse cholesterol transport (RCT) study. J Lipid Res. 2010 Dec;51(12):3443-54.


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