Anacetrapib is a potent and selective CETP inhibitor for rhCETP and C13S CETP mutants with IC50 of 7.9 nM and 11.8 nM, respectively.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Cholesteryl ester transfer protein inhibitor
Product Description
Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3. A potent and selective CETP inhibitor.
Product Properties
ALogP
8.8
Associated Targets(Human)
CETPTchemCholesteryl ester transfer protein (12 Activities)
1.Smith CJ, Ali A, Hammond ML, Li H, Lu Z, Napolitano J, Taylor GE, Thompson CF, Anderson MS, Chen Y et al.. (2011) Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.. J Med Chem, 54 (13):(4880-95). [PMID:21682257]
2.Gutstein DE, Krishna R, Johns D, Surks HK, Dansky HM, Shah S, Mitchel YB, Arena J, Wagner JA. (2012) Anacetrapib, a novel CETP inhibitor: pursuing a new approach to cardiovascular risk reduction.. Clin Pharmacol Ther, 91 (1):(109-22). [PMID:22130116]
3.Kastelein JJ, Besseling J, Shah S, Bergeron J, Langslet G, Hovingh GK, Al-Saady N, Koeijvoets M, Hunter J, Johnson-Levonas AO et al.. (2015) Anacetrapib as lipid-modifying therapy in patients with heterozygous familial hypercholesterolaemia (REALIZE): a randomised, double-blind, placebo-controlled, phase 3 study.. Lancet, 385 (9983):(2153-61). [PMID:25743173]
5.Millar JS, Reyes-Soffer G, Jumes P, Dunbar RL, deGoma EM, Baer AL, Karmally W, Donovan DS, Rafeek H, Pollan L et al.. (2015) Anacetrapib lowers LDL by increasing ApoB clearance in mildly hypercholesterolemic subjects.. J Clin Invest, 125 (6):(2510-2522). [PMID:25961461]
6.Filippatos TD, Kei A, Elisaf MS. (2017) Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?. Diseases, 5 (4):(589-97). [PMID:28961179]
7.Ready JM. (2021) Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP).. J Med Chem, 64 (18):(13212-13214). [PMID:34498872]
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