达塞曲匹 T6048

Product Introduction
Bioactivity


英文名: Dalcetrapib

描述: Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM)，具有增加血浆中HDL 胆固醇含量的作用。

细胞实验: 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)

激酶实验: 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.

体外活性: 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]

体内活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 72 mg/mL (184.8 mM)
Ethanol : 72 mg/mL (184.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: CETP | Inhibitor | HDL cholesterol | inhibit | JTT 705 | JTT705 | RO 4607381 | Cholesteryl ester transfer protein | orally active | Dalcetrapib | RO-4607381

相关产品: Torcetrapib | Evacetrapib | Anacetrapib | Granotapide | CP-532623 | Dirlotapide | NAMI-A | KD-026 | Lomitapide | Lomitapide Mesylate

相关库: Drug Repurposing Compound Library | Bioactive Lipid Compound Library | ReFRAME Related Library | Bioactive Compounds Library Max | Human Metabolite Library | Inhibitor Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

达塞曲匹 T6048信息由TargetMol中国为您提供，如您想了解更多关于达塞曲匹 T6048报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途