Dalcetrapib (JTT-705, RO4607381)

Alias: Dalcetrapib; JTT-705; RO-4607381; RO4607381; RO 4607381; JTT705; JTT 705
Cat No.:V0914 Purity: ≥98%
Dalcetrapib (formerly JTT-705;RO-4607381; JTT705;RO4607381) is a novel, potent and selectiveinhibitor of CETP (Cholesteryl ester transfer protein) with the potential to prevent cardiovascular diseases.
Dalcetrapib (JTT-705, RO4607381) Chemical Structure CAS No.: 211513-37-0
Product category: CETP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Dalcetrapib (formerly JTT-705; RO-4607381; JTT705; RO4607381) is a novel, potent and selective inhibitor of CETP (Cholesteryl ester transfer protein) with the potential to prevent cardiovascular diseases. It inhibits CETP with an IC50 of 0.2 μM thus is able to increase the plasma HDL cholesterol (good cholesterol' ). Dalcetrapib was designed to raise the 'good cholesterol' levels in the blood (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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) enhances pre-β-HDL production in a dose-dependent manner[1]. In HepG2, Dalcetrapib (0-30 μM; 24 h) dose-dependently suppresses the media's CETP activity[3].
ln Vivo
In rabbits, dacletrapib (JTT-705) (30 or 100 mg/kg; po; once daily for three days) considerably raises plasma HDL cholesterol[2]. Neutral sterol, bile acids, and plasma HDL-cholesterol are considerably increased in the feces upon administration of dacletrapib (100 mg/kg; ir; twice daily for 7 days)[1].
Animal Protocol
Animal/Disease Models: Male JW rabbits[2]
Doses: 30 or 100 mg/kg
Route of Administration: Oral administration, one time/day for 3 days
Experimental Results: Increased plasma HDL cholesterol by 27% and 54% at 30 mg/kg and 100 mg/kg, respectively.
References
[1]. Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.
[2]. Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572.
[3]. Huang Z, et al. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H35NO2S
Molecular Weight
389.59
CAS #
211513-37-0
SMILES
CC(C)C(SC1=CC=CC=C1NC(C2(CC(CC)CC)CCCCC2)=O)=O
Chemical Name
S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate
Synonyms
Dalcetrapib; JTT-705; RO-4607381; RO4607381; RO 4607381; JTT705; JTT 705
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5668 mL 12.8340 mL 25.6680 mL
5 mM 0.5134 mL 2.5668 mL 5.1336 mL
10 mM 0.2567 mL 1.2834 mL 2.5668 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • 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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