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经验公式(希尔记法):
C26H25F9N2O4
化学文摘社编号:
分子量:
600.47
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C26H25F9N2O4/c1-4-18-12-21(19-11-15(24(27,28)29)6-7-20(19)37(18)23(39)41-5-2)36(22(38)40-3)13-14-8-16(25(30,31)32)10-17(9-14)26(33,34)35/h6-11,18,21H,4-5,12-13H2,1-3H3/t18-,21+/m1/s1
SMILES string
CCOC(=O)N1[C@H](CC)C[C@H](N(Cc2cc(cc(c2)C(F)(F)F)C(F)(F)F)C(=O)OC)c3cc(ccc13)C(F)(F)F
InChI key
CMSGWTNRGKRWGS-NQIIRXRSSA-N
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D >-70°
color
white
solubility
DMSO: >5 mg/mL
storage temp.
2-8°C
Quality Level
Application
Torcetrapib has been used as a reference standard in the medium chain-lipid based formulations.
Biochem/physiol Actions
Cholesteryl ester transfer protein (CETP) inhibitor.
Torcetrapib is a Cholesteryl ester transfer protein (CETP) inhibitor. CETP normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels (the "good" cholesterol-containing particle) and reduces LDL levels (the "bad" cholesterol). Unfortunately clinical trials were stopped because of excessive all cause mortality. Reasons are still being investigated, but may be related to some off target effects such as an increase in aldosterone secretion not found in some other CETP inhibitors.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ziyun Wang et al.
PloS one, 12(8), e0180772-e0180772 (2017-08-03)
Cholesteryl ester transfer protein (CETP) is a plasma protein that mediates bidirectional transfers of cholesteryl esters and triglycerides between low-density lipoproteins and high-density lipoproteins (HDL). Because low levels of plasma CETP are associated with increased plasma HDL-cholesterol, therapeutic inhibition of
Stephen J Nicholls
Current cardiology reports, 14(3), 245-250 (2012-03-01)
Considerable attention focuses on the ability to develop therapeutic agents that elevate levels of high-density lipoprotein cholesterol (HDL-C). Cholesteryl ester transfer protein (CETP) inhibitors have been developed on the basis of their ability to raise HDL-C to a greater extent
Margaret R Diffenderfer et al.
Journal of lipid research, 53(6), 1190-1199 (2012-04-05)
Cholesteryl ester transfer protein (CETP) facilitates the transfer of HDL cholesteryl ester to triglyceride-rich lipoproteins (TRL). This study aimed to determine the effects of CETP inhibition with torcetrapib on TRL composition and apoB-48 metabolism. Study subjects with low HDL cholesterol
Alexander J M Rennings et al.
Expert opinion on investigational drugs, 17(10), 1589-1597 (2008-09-24)
Despite reduction in low-density lipoprotein cholesterol, there is still a considerable amount of residual atherosclerosis-related disease. Epidemiological and pathophysiological data strongly favour increasing plasma high-density lipoprotein (HDL) cholesterol levels as antiatherogenic therapy, for example with cholesteryl ester transfer inhibition (CETP).
Douglas G Johns et al.
Drugs, 72(4), 491-507 (2012-02-24)
Lowering of serum low-density lipoprotein cholesterol (LDL-C) levels remains the primary aim of lipid management. Much progress has been made in reducing rates of cardiovascular disease morbidity and mortality, largely through increased awareness of lipid-lowering therapies and particularly through the
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