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Torcetrapib

Torcetrapib structure

Torcetrapib 

structure
  • CAS No:

    262352-17-0

  • Formula:

    C26H25F9N2O4

  • Chemical Name:

    Torcetrapib

  • 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

  • Categories:

    Biochemical Engineering  >  Inhibitors

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.

Torcetrapib Basic Attributes

603.49

600.47

4N4457MV2U

DTXSID20180873

C91058

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

Safety Information

NONH for all modes of transport

3

22

Xn

P264, P270, P301+P312, P330, P501

H302

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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