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PZ0170

Sigma-Aldrich

Torcetrapib

≥98% (HPLC)

Synonyme(s) :

(2R,4S)-4-((3,5-Bis-trifluoromethylbenzyl)methoxycarbonylamino)-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester, CP-529,414, CP-529414

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About This Item

Formule empirique (notation de Hill):
C26H25F9N2O4
Numéro CAS:
262352-17-0
Poids moléculaire :
600.47
Numéro MDL:
MFCD09260777
Code UNSPSC :
12352200
ID de substance PubChem :
329823744
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Activité optique

[α]/D >-70°

Couleur

white

Solubilité

DMSO: >5 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

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

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

Clé InChI

CMSGWTNRGKRWGS-NQIIRXRSSA-N

Application

Torcetrapib has been used as a reference standard in the medium chain-lipid based formulations.

Actions biochimiques/physiologiques

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.

Pictogrammes

Exclamation mark
GHS07

Mention d'avertissement

Warning

Mentions de danger

H302

Classification des risques

Acute Tox. 4 Oral

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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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
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
Shenping Liu et al.
The Journal of biological chemistry, 287(44), 37321-37329 (2012-09-11)
Human plasma cholesteryl ester transfer protein (CETP) transports cholesteryl ester from the antiatherogenic high-density lipoproteins (HDL) to the proatherogenic low-density and very low-density lipoproteins (LDL and VLDL). Inhibition of CETP has been shown to raise human plasma HDL cholesterol (HDL-C)
Philip J Barter et al.
Circulation, 124(5), 555-562 (2011-08-02)
High-density lipoproteins have antidiabetic properties in vitro. Furthermore, elevated high-density lipoprotein levels accompanying a genetic deficiency of cholesteryl ester transfer protein are associated with decreased levels of plasma glucose. We now investigate effects on glucose homeostasis of inhibiting cholesteryl ester
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).
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Protocoles

CETP Activity Assay Kit Protocol

The CETP Activity Assay Kit enables the detection of CETP-mediated transfer of neutral lipids.

Contenu apparenté

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