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Dalcetrapib

Catalog No. T6048 CAS 211513-37-0

Synonyms: JTT-705, 达塞曲匹, RO4607381

Dalcetrapib, a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.

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Dalcetrapib, CAS 211513-37-0

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Purity: 98%

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Description	Dalcetrapib, a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol.
Targets&IC50	rhCETP: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]
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	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.(Only for Reference)

Synonyms	JTT-705, 达塞曲匹, RO4607381
Molecular Weight	389.6
Formula	C23H35NO2S
CAS No.	211513-37-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 72 mg/mL (184.8 mM)

Ethanol: 72 mg/mL (184.8 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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. 3. Huang Z, et al. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219. 4. Zhang B, et al. Arterioscler Thromb Vasc Biol. 2004, 24(10), 1910-1915. 5. Derks M, et al. Br J Clin Pharmacol. 2010, 70(6), 825-833.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Cardiovascular Disease Compound Library Anti-Obesity Compound Library Lipid Metabolism Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Drug Repurposing Compound Library Bioactive Lipid Compound Library Anti-Cancer Drug Library

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Keywords

Dalcetrapib 211513-37-0 代谢 CETP Inhibitor HDL cholesterol inhibit RO-4607381 JTT-705 RO 4607381 Cholesteryl ester transfer protein orally active JTT705 JTT 705 RO4607381 inhibitor

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