Anacetrapib (MK-0859)RhCETP/mutant CETP(C13S) inhibitor CAS# 875446-37-0 |
2D Structure
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
Cas No. | 875446-37-0 | SDF | Download SDF |
PubChem ID | 11556427 | Appearance | Powder |
Formula | C30H25F10NO3 | M.Wt | 637.51 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | MK-0859 | ||
Solubility | DMSO : ≥ 100 mg/mL (156.86 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | (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 | ||
SMILES | CC1C(OC(=O)N1CC2=C(C=CC(=C2)C(F)(F)F)C3=CC(=C(C=C3OC)F)C(C)C)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F | ||
Standard InChIKey | MZZLGJHLQGUVPN-HAWMADMCSA-N | ||
Standard InChI | InChI=1S/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Anacetrapib is a potent, selective, reversible inhibitor of rhCETP and mutant CETP(C13S) with IC50 values of 7.9 nM and 11.8 nM, respectively. | |||||
Targets | rhCETP | mutant CETP(C13S) | ||||
IC50 | 7.9 nM | 11.8 nM |
Anacetrapib (MK-0859) Dilution Calculator
Anacetrapib (MK-0859) Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.5686 mL | 7.843 mL | 15.686 mL | 31.3721 mL | 39.2151 mL |
5 mM | 0.3137 mL | 1.5686 mL | 3.1372 mL | 6.2744 mL | 7.843 mL |
10 mM | 0.1569 mL | 0.7843 mL | 1.5686 mL | 3.1372 mL | 3.9215 mL |
50 mM | 0.0314 mL | 0.1569 mL | 0.3137 mL | 0.6274 mL | 0.7843 mL |
100 mM | 0.0157 mL | 0.0784 mL | 0.1569 mL | 0.3137 mL | 0.3922 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Anacetrapib, also known as MK-0859, is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) that exhibits strong inhibition against CETP-mediated transfer of cholesteryl esters and triglycerides with values of inhibition constant IC50 of 16 nM and 29 nM respectively. Anacetrapib is mainly metabolized by CYP3A4 through O-demethylation, hydroxylation on the biphenyl moiety and hydroxylation on the isopropyl side chain resulting in three oxidative metabolites M1, M2 and M3 respectively. Anacetrapib is being investigated for the treatment of primary hypercholesterolemia and mixed hyperlipidemia due to its impressive effects to lower low-density lipoprotein (LDL) cholesterol levels and increase high-density lipoprotein (HDL) cholesterol levels without any associated major adverse events.
Reference
Tan EY, Hartmann G, Chen Q, Pereira A, Bradley S, Doss G, Zhang AS, Ho JZ, Braun MP, Dean DC, Tang W, Kumar S. Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys. Drug Metab Dispos. 2010;38(3):459-473.
Kumar S, Tan EY, Hartmann G, Biddle Z, Bergman AJ, Dru J, Ho JZ, Jones AN, Staskiewicz SJ, Braun MP, Karanam B, Dean DC, Gendrano IN, Graves MW, Wagner JA, Krishna R. Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans. Drug Metab Dispos. 2010;38(3):474-483
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Efficacy and safety after cessation of treatment with the cholesteryl ester transfer protein inhibitor anacetrapib (MK-0859) in patients with primary hypercholesterolemia or mixed hyperlipidemia.[Pubmed:21982664]
Am Heart J. 2011 Oct;162(4):708-16.
This report describes the lipid and safety data collected during an off-drug period that followed 8 weeks of treatment with the cholesteryl ester transfer protein inhibitor, anacetrapib (ANA). A total of 589 patients with primary hypercholesterolemia or mixed hyperlipidemia were randomized to placebo, atorvastatin (ATV) 20 mg, and varying doses of ANA, provided as monotherapy or coadministered with ATV 20 mg daily. Patients were treated for 8 weeks, followed by an 8-week follow-up period, during which ANA was switched to placebo. At week 16 (8 weeks after ANA was stopped), persistent reductions in low-density lipoprotein cholesterol (LDL-C) were evident for the monotherapy groups receiving ANA 150 and 300 mg (-9.3% and -15.3%, respectively), and residual increases in high-density lipoprotein cholesterol (HDL-C) were observed for the monotherapy groups receiving ANA 40 mg (18.6%), 150 mg (40.5%), and 300 mg (43.4%). The effects on apolipoprotein B and apolipoprotein A-I were consistent with the changes observed for LDL-C and HDL-C, respectively. Corresponding residual changes in LDL-C and HDL-C were also noted in the ATV coadministration groups at the similar doses of ANA compared with ATV 20 mg alone. Residual plasma drug levels accompanied by reductions in cholesteryl ester transfer protein activity were observed at week 16 and may account for the alterations in plasma lipids 8 weeks after cessation of ANA.