Dalcetrapib (JTT-705, RO4607381)

Catalog No.S2772

Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.

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Dalcetrapib (JTT-705, RO4607381) Chemical Structure

Dalcetrapib (JTT-705, RO4607381) Chemical Structure
Molecular Weight: 389.59

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Dalcetrapib (JTT-705, RO4607381) is available in the following compound libraries:

Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.
Targets rhCETP [1]
IC50 0.2 μM
In vitro 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. [1] Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM. [2] Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner. [3]
In vivo Treatment 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. [1] 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. [2] 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. [4]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Inhibition of rhCETP and C13S CETP-mediated transfer of CE from HDL to LDL 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: [3]

Cell lines HepG2 cells
Concentrations 0-30 μM
Incubation Time 24 hours
Method 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.

Animal Study: [1]

Animal Models Syrian hamsters
Formulation 0.5% methylcellulose
Dosages 100 mg/kg
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Niesor EJ, et al. J Lipid Res. 2010, 51(12), 3443-3454.

[2] Shinkai H, et al. J Med Chem. 2000, 43(19), 3566-3572.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02525939 Recruiting Acute Coronary Syndrome DalCor Pharmaceuticals|The Montreal Health Innovations Co  ...more DalCor Pharmaceuticals|The Montreal Health Innovations Coordinating Center (MHICC)|Medpace, Inc.|Roche Molecular Systems, Inc April 2016 Phase 3
NCT01516541 Completed Cardiovascular Disease, Coronary Heart Disease, Dyslipidemia, Peripheral Arterial Disease (PAD) Hoffmann-La Roche January 2012 Phase 3
NCT01476267 Completed Healthy Volunteer Hoffmann-La Roche October 2011 Phase 1
NCT01363999 Completed Healthy Volunteer Hoffmann-La Roche June 2011 Phase 1
NCT01323153 Completed Coronary Heart Disease Hoffmann-La Roche March 2011 Phase 3

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Chemical Information

Download Dalcetrapib (JTT-705, RO4607381) SDF
Molecular Weight (MW) 389.59
Formula

C23H35NO2S

CAS No. 211513-37-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 78 mg/mL (200.21 mM)
Ethanol 78 mg/mL (200.21 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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