CETP-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/CETP.html CETPCholesteryl ester transfer proteinCholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl esters from theatheroprotective high density lipoprotein (HDL) to the proatherogenic low density lipo

2、protein cholesterol (LDL) and very lowdensity lipoprotein cholesterol (VLDL) leading to lower levels of HDL but raising the levels of proatherogenic LDL and VLDL. CETPinhibitors are a class of drugs that targets the CETP enzyme to significantly increase serum HDL-C and decrease LDL-C levels.Inhibiti

3、on of CETP is considered a potential approach to treat dyslipidemia.Alterations of CETP activity levels can be caused by single-base polymorphisms as well as by alternative splicing. Several commonvariants in CETP have been reported to be associated with variation in plasma lipid levels, CAD risk an

4、d/or CETP mass/activity. Therare genetic variants in the CETP gene also contribute to the phenotypic variation of HDL-C in the general population.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/CETP.html CETP HYPERLINK https:/www.MedChemE/Targets/CETP.html HYPERLINK https:/www.MedChemE/Targets/

5、CETP.html Inhibitors HYPERLINK https:/www.MedChemE/Anacetrapib.html Anacetrapib(MK-0859) Cat. No.: HY-12090 HYPERLINK https:/www.MedChemE/anacetrapib-d3.html Anacetrapib-d3Cat. No.: HY-12090SAnacetrapib is a potent CETP inhibitor, withIC s of 7.92.5 nM and 11.81.9 nM for rhCETP and50C13S CETP mutant

6、, respectively.Anacetrapib-d3 is the deuterium labeledAnacetrapib. Anacetrapib is a potent CETPinhibitor, with IC s of 7.92.5 nM and 11.81.950nM for rhCETP and C13S CETP mutant, respectively.Purity: 99.62%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No

7、Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/bms-795311.html BMS-795311 HYPERLINK https:/www.MedChemE/bms-795311.html HYPERLINK https:/www.MedChemE/cetp-in-3.html CETP-IN-3Cat. No.: HY-19614 Cat. No.: HY-128338BMS-795311 is a potent and orally bioavailableinhibitor of cholesteryl est

8、er transfer protein(CETP), with IC s of 4 nM in an enzyme-based50scintillation proximity assay (SPA) and 0.22 M ina human whole plasma assay (hWPA), respectively.CETP-IN-3 (Compound 13) is an small moleculeinhibitor of the plasma glycoprotein cholesterolester transfer protein (CETP), elevating HDL-C

9、through inhibition of CETP.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cetp-in-4.html CETP-IN-4 HYPERLINK https:/www.MedChemE/cetp-in-4.html HYPERLINK https:/www.MedChemE/ckd-519.html

10、 CKD-519Cat. No.: HY-142643 Cat. No.: HY-116078CETP-IN-4 is a cholesteryl ester transfer protein(CETP) inhibitor.CKD-519 is a selective and potent cholesteryl estertransfer protein (CETP) inhibitor, which inhibitsCETP-mediated transfer of cholesteryl ester inhuman serum with an IC of 2.3 nM.50Purity

11、: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cp-532623.html CP-532623 HYPERLINK https:/www.MedChemE/cp-532623.html HYPERLINK https:/www.MedChemE/Dalcetrapib.html DalcetrapibCat. No.: HY-123039(JTT-705; RO46

12、07381) Cat. No.: HY-14950CP-532623 is a CETP inhibitor and elevateshigh-density lipoprotein cholesterolion. CP-532623is a close structural analogue of Torcetrapib.CP-532623 has highly lipophilic properties.Dalcetrapib (JTT-705; RO-4607381) is a rhCETPinhibitor with IC50 of 0.2 M that increases thepl

13、asma HDL cholesterol. IC50 value: 0.2 uM Target:CETP in vitro: Dalcetrapib modulates CETPactivity.Purity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.42%Clinical Data: Phase 3Size: 10 mM 1 mL, 50 mg, 100 mg, 250 mg HYPERLINK https:/www.MedChemE/Evacetrapib.html

14、 Evacetrapib HYPERLINK https:/www.MedChemE/Evacetrapib.html HYPERLINK https:/www.MedChemE/mk-8262.html MK-8262(LY2484595) Cat. No.: HY-13327Cat. No.: HY-132303Evacetrapib is a potent and selective of CETPinhibitor, which inhibits human recombinant CETPprotein (IC 5.5 nM) and CETP activity in human50

15、plasma (IC 36 nM) in vitro.50MK-8262 is an orally active and potent cholesterylester transfer protein (CETP) inhibitor with anIC of 53 nM and a logD of 5.3.50Purity: 99.42%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

16、 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/tap311.html TAP311Cat. No.: HY-107997 HYPERLINK https:/www.MedChemE/Torcetrapib.html Torcetrapib(CP-529414) Cat. No.: HY-12089TAP311 is a cholesteryl ester transfer protein(CETP) inhibitor with an IC of 62 nM.50Torcetrapib (CP-529414) is a selective, potentcholesteryl ester