Dalcetrapib NEW
| Price | $37 | $57 | $72 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Dalcetrapib | CAS No.: 211513-37-0 |
| Purity: 97.98% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Dalcetrapib |
| Description | Dalcetrapib (RO4607381), a rhCETP inhibitor (IC50=0.2 μM), increases the plasma HDL cholesterol. |
| 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) |
| 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. |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 72 mg/mL (184.8 mM) Ethanol : 72 mg/mL (184.8 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | CETP | Inhibitor | HDL cholesterol | inhibit | JTT 705 | JTT705 | RO 4607381 | Cholesteryl ester transfer protein | orally active | Dalcetrapib | RO-4607381 |
| Inhibitors Related | Anacetrapib | Granotapide | BMS-212122 | KD-026 | NAMI-A | Lomitapide | Dirlotapide | Obicetrapib |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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