Torcetrapib
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Torcetrapib
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CAS No:
262352-17-0
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Formula:
C26H25F9N2O4
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Chemical Name:
Torcetrapib
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Synonyms:
1(2H)-Quinolinecarboxylic acid,4-[[[3,5-bis(trifluoromethyl)phenyl]methyl](methoxycarbonyl)amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-,ethyl ester,(2R,4S)-;CP 529414;Torcetrapib;(2R,4S)-4-[(3,5-Bis-trifluoromethylbenzyl)methoxycarbonylamino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester;(2R,4S)-4-[[3,5-Bis(trifluoromethyl)benzyl]methoxycarbonylamino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester;(-)-Torcetrapib
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CAS No:
Description
Torcetrapib(CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma.IC50 value: 37 nM [1]Target: CETP inhibitorin vitro: Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated by calcium channel as calcium channel blockers completely blocks torcetrapib-induced corticoid release and calcium increase. Torcetrapib (1 μM) significantl
Torcetrapib is a member of quinolines, a carbamate ester and a member of (trifluoromethyl)benzenes. It has a role as an anticholesteremic drug and a CETP inhibitor.|Torcetrapib (CP-529414, Pfizer) was developed to treat hypercholesterolemia but its development was halted in 2006 when phase III studies showed excessive mortality in the treatment group receiving a combination of atorvastatin and the study drug.|Torcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor that reduces the heterotypic transfer of cholesteryl ester from HDL to LDL and/or VLDL. Torcetrapib failed in phase III trials due to excess deaths.
Characteristics
59.1
7.76
white
1.4±0.1 g/cm3
54-58 °C
504.8±50.0 °C at 760 mmHg
259.1±30.1 °C
1.512
DMSO: >5mg/mL
Store at RT
Drug Information
Investigated for use/treatment in peripheral vascular disease and hyperlipidemia.
Substances used to lower plasma cholesterol levels. (See all compounds classified as Anticholesteremic Agents.)
Torcetrapib is an inhibitor of cholesteryl ester-transfer protein (CETP) that increases high-density lipoprotein (HDL) cholesterol levels. The drug increases HDL-cholesterol and apolipoprotein A-I levels and decreases LDL-cholesterol and apolipoprotein B levels. The effect is showed in monotherapy and when administered in combination with statins.
CP 529,414
Torcetrapib Use and Manufacturing
Cholesteryl ester transfer protein (CETP) inhibitor. Antilipemic; antiatherosclerotic.
Computed Properties
Molecular Weight:600.5
XLogP3:7
Hydrogen Bond Acceptor Count:13
Rotatable Bond Count:7
Exact Mass:600.16706074
Monoisotopic Mass:600.16706074
Topological Polar Surface Area:59.1
Heavy Atom Count:41
Complexity:889
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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