Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that promotes reverse cholesterol transport via the exchange of cholesteryl ester (CE) and triglyceride (TG) among lipoproteins. Cholesteryl ester transfer protein (CETP) promotes reverse cholesterol transport via exchange of cholesteryl ester and triglyceride among lipoproteins. CETP has a central role in lipoprotein metabolism. CETP, a hydrophobic plasma glycoprotein, is a promising target for raising circulating HDL cholesterol (HDL-C) concentrations in humans. CETP is secreted primarily from the liver and plays a critical role in HDL metabolism by facilitating the exchange of cholesteryl esters (CE) from HDL for triglycerides (TG) in apoB-containing lipoproteins, such as LDL and VLDL. CETP catalyses the exchange of cholesteryl ester and triglyceride between HDL and apoB containing lipoprotein particles. The role of CETP in modulating plasma HDL cholesterol levels in humans is well established and there have been significant efforts to develop CETP inhibitors to increase HDL cholesterol for the treatment of coronary artery disease.


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BMS 795311

BMS-795311 is a potent and orally available CETP inhibitor with IC50 of 3.8 nM, inhibits cholesteryl ester (CE) transfer with IC50 of 0.22 uM; inhibits CE transfer activity at an oral dose of 1 mg/kg in human CETP/apoB-100 dual transgenic mice and increased HDL cholesterol content and size comparable to Torcetrapib in moderately-fat fed hamsters.

  • CAS Number: 939390-99-5
  • MF: C33H23F10NO3
  • MW: 671.525
  • Catalog: CETP
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 620.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 328.8±31.5 °C

CETP-IN-3

CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitory activity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively[1].

  • CAS Number: 939391-31-8
  • MF: C30H24F12N2O4
  • MW: 704.50
  • Catalog: CETP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(10β)-10,18-Epoxyros-15-ene-7,18-dione

Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein[1][2][3].

  • CAS Number: 508-71-4
  • MF: C20H28O3
  • MW: 316.43
  • Catalog: CETP
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 449.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 196.2±28.8 °C

Evacetrapib (LY2484595)

Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

  • CAS Number: 1186486-62-3
  • MF: C31H36F6N6O2
  • MW: 638.647
  • Catalog: CETP
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 680.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 365.1±34.3 °C

Anacetrapib

Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.

  • CAS Number: 875446-37-0
  • MF: C30H25F10NO3
  • MW: 637.508
  • Catalog: CETP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 555.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 289.6±30.1 °C

Torcetrapib

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) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines [2].in vivo: Torcetrapib (< 100 mg, daily) changes the plasma distribution of CETP, as the apparent molecular weight of the CETP has shifted to a larger form, by 2 hours after the dose in healthy young subjects. Torcetrapib treatment with 10 mg, 30 mg, 60 mg, and 120 mg daily and 120 mg twice daily results in 16%, 28%, 62%, 73%, and 91% increases in plasma HDL-C, respectively, with no significant changes in TPC in healthy young subjects. [1] Torcetrapib results in an increase of 72.1% in high-density lipoprotein cholesterol and a decrease of 24.9% in low-density lipoprotein cholesterol, in addition to an increase of 5.4 mm Hg in systolic blood pressure, a decrease in serum potassium, and increases in serum sodium, bicarbonate, and aldosterone, in patients at high cardiovascular risk after 12 months' treatment [3]. Torcetrapib (90 mg/kg/day) results in a 70% inhibition of CE transfer in rabbits fed an atherogenic diet. Torcetrapib (90 mg/kg/day) increases mean HDL-C levels by above 3-fold and apoA-I levels by 2.5-fold in plasma in rabbits fed an atherogenic diet. Torcetrapib-treated animal has a multiple-fold increase in HDL-C AUC and a corresponding reduction in aortic lesion area with 60% reduction of aortic free cholesterol (FC) and cholesteryl ester (EC) in rabbits fed an atherogenic diet. Torcetrapib-treated rabbits stimulate free cholesterol efflux to a significantly greater extent than does sera from control rabbits [4].

  • CAS Number: 262352-17-0
  • MF: C26H25F9N2O4
  • MW: 600.47
  • Catalog: CETP
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 504.8±50.0 °C at 760 mmHg
  • Melting Point: 54-58ºC
  • Flash Point: 259.1±30.1 °C

CETP-IN-4

CETP-IN-4 is a cholesteryl ester transfer protein (CETP) inhibitor.

  • CAS Number: 1648889-70-6
  • MF: C36H28F9N3O4
  • MW: 737.61
  • Catalog: CETP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CP-532623

CP-532623 is a CETP inhibitor and elevates high-density lipoprotein cholesterolion. CP-532623 is a close structural analogue of Torcetrapib. CP-532623 has highly lipophilic properties[1][2][3].

  • CAS Number: 261947-38-0
  • MF: C27H27F9N2O3
  • MW: 598.50
  • Catalog: CETP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dalcetrapib

Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. IC50 value: 0.2 uM [1]Target: CETPin vitro: Dalcetrapib modulates CETP activity. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-β-HDL formation in human plasma is unchanged by Dalcetrapib ≤3 μM and increased at 10 μM. Dalcetrapib statistically and significantly increases pre-β-HDL formation [1]. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM [2]. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner [3].in vivo: Treatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [3H]cholesterol-labeled autologous macrophages Dalcetrapib significantly increases fecal elimination of both [3H]neutral sterols and [3H]bile acids. Dalcetrapib increases plasma HDL-[3H]cholesterol [1]. Dalcetrapib has 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits [2].

  • CAS Number: 211513-37-0
  • MF: C23H35NO2S
  • MW: 389.59500
  • Catalog: CETP
  • Density: 1.066 g/cm3
  • Boiling Point: 528.912ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 273.676ºC

MK-8262

MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research[1].

  • CAS Number: 1432054-03-9
  • MF: C35H25F9N2O5
  • MW: 724.57
  • Catalog: CETP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CKD-519

CKD-519 is a selective and potent cholesteryl ester transfer protein (CETP) inhibitor, which inhibits CETP-mediated transfer of cholesteryl ester in human serum with an IC50 of 2.3 nM[1].

  • CAS Number: 1402796-27-3
  • MF: C31H34F7NO3
  • MW: 601.60
  • Catalog: CETP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A