To enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
| Cas No.: | 875446-37-0 |
| Chemical Name: | Anacetrapib |
| Synonyms: | Anacetrapib;(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one;(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one;Anacetrapib (MK-0859);MK0859;MK-0859;UNII-P7T269PR6S;P7T269PR6S;(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-[[4'-fluoro-5'-isopropyl-2'-methoxy-4-(trifluoromethyl)biphenyl-2-yl]methyl]-4-methyl-1,3-oxazolidin-2-one;Anacetrapib [USAN:INN];Anacetrapib (JAN/USAN);cc-7 |
| SMILES: | FC(C1C([H])=C(C(F)(F)F)C([H])=C(C=1[H])[C@]1([H])[C@]([H])(C([H])([H])[H])N(C(=O)O1)C([H])([H])C1C([H])=C(C(F)(F)F)C([H])=C([H])C=1C1C(=C([H])C(=C(C([H])(C([H])([H])[H])C([H])([H])[H])C=1[H])F)OC([H])([H])[H])(F)F |
| Formula: | C30H25F10NO3 |
| M.Wt: | 637.5084 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively. |
| In Vivo: | Hamsters are given Anacetrapib for 7 days before injection of [3H]cholesterol-labeled macrophages (day 0). Treatment with Anacetrapib leads to significant increases in HDL-C levels at day 0. At day 3, [3H]cholesterol radioactivity in the HDL fraction is significantly increased from control values for Anacetrapib[1]. Anacetrapib (ANA) treatment modestly elevates serum total serum cholesterol levels ~10% (p<0.05) and increases serum LDL-C by 26% (p<0.05) as compared to vehicle control[2]. After an intravenous dose of 0.5 mg/kg, the mean values for systemic plasma clearance, steady-state volume of distribution, and terminal half-life are 2.3 mL/min/kg, 1.1 L/kg, and 12 h, respectively. After oral dosing at 5 mg/kg, the bioavailability of Anacetrapib is 38%. Exposures (AUC) increases in a less than dose-proportional manner from 23 μM•h at 5 mg/kg to 362 μM•h at 500 mg/kg. In this dose range, the peak plasma level (Cmax) ranges from 5 to 26 μM and the time to reach peak plasma level (Tmax) ranged from 3 to 4.5 h[3]. |
| In Vitro: | Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2 (P<0.001 for concentrations equal to and higher than 0.1 µM). Excess Anacetrapib (25 µM) decreases the amount of [14C]Torcetrapib (0.25 µM) binds to immobilized rhCETP by 82% and 60%, respectively. Anacetrapib decreases pre-β-HDL formation by more than 46% (P<0.001) at all concentrations tested (0.1, 1, 3, and 10 µM)[1]. A significant reduction of PCSK9 promoter activity by Anacetrapib (ANA) is detected at 3 µM concentration (−22%, p<0.01) and further lowered to 68% of control at 10 µM. Likewise, luciferase activity of B11 cells are decreased by Anacetrapib at 3 µM concentration and reached to a maximal reduction of 38% of control at 10 µM. At 10 µM concentration, Anacetrapib loweres PCSK9 mRNA level to 60% of control and LDLR mRNA level to 67% of control[2]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
|
|
|
| 2018-0101 |
|
| 2018-0101 |
|
| 2018-0101 |
|