Home Metabolism CETP inhibitor Dalcetrapib (JTT-705) For research use only.

Dalcetrapib (JTT-705)

Synonyms: RO4607381

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

Dalcetrapib (JTT-705) Chemical Structure

Dalcetrapib (JTT-705) Chemical Structure

CAS No. 211513-37-0

Purity & Quality Control

Batch: S277201 DMSO]78 mg/mL]false]Ethanol]78 mg/mL]false]Water]Insoluble]false Purity: 99.73%
99.73

Dalcetrapib (JTT-705) Related Products

Signaling Pathway

CETP Signaling Pathways

CETP Signaling Pathway

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]
0.2 μM
In vitro
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]
Kinase Assay 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 Research 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.
In Vivo
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]
Animal Research Animal Models Syrian hamsters
Dosages 100 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04676867 Completed
Covid19
DalCor Pharmaceuticals|The Montreal Health Innovations Coordinating Center (MHICC)|Covance
 January 11 2021 Phase 2
NCT01363999 Completed
Healthy Volunteer
Hoffmann-La Roche
 June 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 389.59 Formula

C23H35NO2S
CAS No. 211513-37-0 SDF Download Dalcetrapib (JTT-705) SDF
Smiles CCC(CC)CC1(CCCCC1)C(=O)NC2=CC=CC=C2SC(=O)C(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (200.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 78 mg/mL

Water : Insoluble


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In vivo
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