A CETP inhibitor
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Anacetrapib

Item No. 21558

Technical Information
Formal Name
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[4'-fluoro-2'-methoxy-5'-(1-methylethyl)-4-(trifluoromethyl)[1,1'-biphenyl]-2-yl]methyl]-4-methyl-2-oxazolidinone
CAS Number
875446-37-0
Synonyms
  • MK-0859
Molecular Formula
C30H25F10NO3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
255, 285 nm
SMILES
FC1=C(C(C)C)C=C(C2=C(CN3C(O[C@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)[C@@H]3C)=O)C=C(C(F)(F)F)C=C2)C(OC)=C1
InChi Code
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
InChi Key
MZZLGJHLQGUVPN-HAWMADMCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Anacetrapib is an inhibitor of cholesterol ester transfer protein (CETP) with IC50 values of 17 and 15 nM for CETP-dependent transfer of cholesterol esters and triglycerides, respectively.1 It decreases plasma levels of LDL and triglycerides, reduces atherosclerotic lesion sizes, and increases HDL levels in the E3L.CETP mouse model of atherosclerosis.2 Anacetrapib (150 mg/kg) increases HDL levels by 2-fold and lowers LDL and fasting plasma triglyceride levels in rhesus macaques.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ranalletta, M., Bierilo, K.K., Chen, Y., et alBiochemical characterization of cholesteryl ester transfer protein inhibitors. J. Lipid. Res. 51(9), 2739-2752 (2010).

    2. van der Tuin, S.J., Kühnast, S., Berbée, J.F., et alAnacetrapib reduces (V)LDL cholesterol by inhibition of CETP activity and reduction of plasma PCSK9. J. Lipid Res. 56(11), 2085-2093 (2015).

    3. McLaren, D.G., Previs, S.F., Phair, R.D., et alEvaluation of CETP activity in vivo under non-steady-state conditions: Influence of anacetrapib on HDL-TG flux. J. Lipid Res. 57(3), 398-409 (2016).