875446-37-0
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-{[4'-fluoro-2'-methoxy-5'-(propan-2-yl)-4-(trifluoromethyl)biphenyl-2-yl]methyl}-4-methyl-1,3-oxazolidin-2-one
CAS: 875446-37-0
Molecular Formula: C30H25F10NO3
875446-37-0 - Names and Identifiers
| Name | (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-{[4'-fluoro-2'-methoxy-5'-(propan-2-yl)-4-(trifluoromethyl)biphenyl-2-yl]methyl}-4-methyl-1,3-oxazolidin-2-one |
| Synonyms | Mk0859 Mk-0859 Anacetrapib Unii-p7T269pr6s Anacetrapib(MK0859) Anacetrapib (With 3 Ints.) (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 (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-{[4'-fluoro-2'-methoxy-5'-(propan-2-yl)-4-(trifluoromethyl)biphenyl-2-yl]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-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one 2-Oxazolidinone, 5-[3,5-bis(trifluoroMethyl)phenyl]-3-[[4'-fluoro-2'-Methoxy-5'-(1-Methylethyl)-4-(trifluoroMethyl)[1,1'-biphenyl]-2-yl]Methyl]-4-Methyl-, (4S,5R)- |
| CAS | 875446-37-0 |
| EINECS | 1312995-182-4 |
| InChI | InChI=1/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 |
875446-37-0 - Physico-chemical Properties
| Molecular Formula | C30H25F10NO3 |
| Molar Mass | 637.51 |
| Density | 1.345 |
| Boling Point | 555.3±50.0 °C(Predicted) |
| Flash Point | 289.641°C |
| Solubility | 127 mg/mL in DMSO <1 mg/mL in Water 127 mg/mL in Ethanol. |
| Vapor Presure | 0mmHg at 25°C |
| pKa | -2.30±0.60(Predicted) |
| Storage Condition | -20℃ |
| Refractive Index | 1.494 |
| Use | A potent and selective CETP inhibitor. |
| In vitro study | Anacetrapib selectively and efficiently inhibits recombinant human CETP and C13S mutant CETP with IC50 of 7.9 and 11.8 nM, respectively. When Anacetrapib is taken together with statins, it not only increases HDL-cholesterol levels, but also further reduces LDL-cholesterol levels. Anacetrapib significantly reduced the transition of CE from HDL3 to HDL2 in a dose-dependent manner. Anacetrapib did not affect the binding number of [14 C]-dalcetrapibthiol to human recombinant CETP. |
| In vivo study | Anacetrapib was used to treat abnormal hamster models at a dose of 60 mg/kg every day for 2 weeks. Compared with the control group, CETP activity decreased by 94% and HDL-cholesterol increased by 47%, non-HDL cholesterol concentrations were not affected. In addition, Anacetrapib promoted reverse cholesterol transport in macrophages, resulting in a 30% increase in fecal cholesterol content. Anacetrapib treated hamster HDL showed increased SR-B1 and ABCG1 regulated effluent compared to the control group. Treated orally at a dose of 10 mg/kg [ |
875446-37-0 - Introduction
Anacetrapib (MK-0859) is an effective, selective and reversible inhibitor of rhCETP and mutant CETP(C13S). IC50 is 7.9 nM and 11.8 nM respectively, which improves HDL-C, reduces LDL-C, and does not increase aldosterone and blood pressure. Phase 3.
Last Update：2022-10-16 17:29:32
875446-37-0 - Reference Information
| biological activity | Anacetrapib (MK-0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitors, IC50 were 7.9 nM and 11.8 nM, increased by HDL-C, decreased by LDL-C, did not increase aldosterone and blood pressure. Phase 3. |
| Target | Value |
| rhCETP | 7.9 nM |
| Mutant CETP (C13S) | 11.8 nM |
Last Update：2024-04-09 20:52:54
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CAS: 875446-37-0
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