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CKD-519

Chemical Structure : CKD-519

CAS No.: 1402796-27-3

CKD-519 (Rocacetrapib, CKD519)

Catalog No.: PC-35463Not For Human Use, Lab Use Only.

CKD-519 (Rocacetrapib, CKD519) is a potent, selective cholesteryl ester transfer protein (CETP) inhibitor, inhibits the CETP-mediated transfer of cholesteryl ester in human serum with IC50 of 2.3 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

CKD-519 (Rocacetrapib, CKD519) is a potent, selective cholesteryl ester transfer protein (CETP) inhibitor, inhibits the CETP-mediated transfer of cholesteryl ester in human serum with IC50 of 2.3 nM.
CKD-519 (Rocacetrapib) exhibites a maximum of 70%-86% inhibition of CETP activity and 25%-48% increase of HDL-C levels after two weeks of oral administration of 1, 3, or 10 mg/kg in transgenic mice expressing human CETP/apolipoprotein AI.
CKD-519 (Rocacetrapib, CKD519) is being developed for the treatment of dyslipidemia to raise high-density lipoprotein cholesterol.

Physicochemical Properties

M.Wt 601.606
Formula C31H34F7NO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5,5-dimethylcyclohex-1-en-1-yl}methyl)-4-methyl-1,3-oxazolidin-2-one

References

1. Kim CO, et al. Drug Des Devel Ther. 2016 Nov 15;10:3763-3770. eCollection 2016.

2. Lee S. Abstract 11228: a novel and potent CETP inhibitor, CKD-519 exerts strong HDL increment and anti-atherosclerotic effects. Circulation. 2013;128(Suppl 22):A11228.

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