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Purity: ≥98%
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.
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].
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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].
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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. |
Molecular Formula |
C23H35NO2S
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Molecular Weight |
389.59
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CAS # |
211513-37-0
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(C)C(SC1=CC=CC=C1NC(C2(CC(CC)CC)CCCCC2)=O)=O
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Chemical Name |
S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate
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Synonyms |
Dalcetrapib; JTT-705; RO-4607381; RO4607381; RO 4607381; JTT705; JTT 705
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.42 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30 mg/mL |
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.
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.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04676867 | Completed Has Results | Drug: Dalcetrapib Other: Placebo |
Covid19 | DalCor Pharmaceuticals | January 11, 2021 | Phase 2 |
NCT05918861 | Recruiting | Drug: Dalcetrapib Drug: Placebo |
Acute Coronary Syndrome | DalCor Pharmaceuticals | October 3, 2023 | Phase 3 |
NCT01363999 | Completed Has Results | Drug: atorvastatin Drug: dalcetrapib |
Healthy Volunteer | Hoffmann-La Roche | June 2011 | Phase 1 |
NCT01516541 | Completed | Drug: Placebo Drug: dalcetrapib |
Cardiovascular Disease, Coronary Heart Disease, Dyslipidemia, Peripheral Arterial Disease (PAD) |
Hoffmann-La Roche | January 2012 | Phase 3 |