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Description: Potent cholesteryl ester transfer protein (CETP) inhibitor
Chemical Name: N-[(1R)-1-[3-(Cyclopropyloxy)-4-fluorophenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide
Purity: ≥98% (HPLC)
Biological Activity
Potent cholesteryl ester transfer protein (CETP) inhibitor (IC50 = 4 nM in an enzyme-based scintillation proximity assay). Inhibits cholesteryl ester transfer and increases HDL-C levels in vivo. Orally bioavailable.
Technical Data
| M. Wt | 671.52 |
| Formula | C33H23F10NO3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 939390-99-5 |
| PubChem ID | 23582473 |
| InChI Key | UBJMOTPQBCKENW-WJOKGBTCSA-N |
| Smiles | FC1=CC(OC(F)(F)C(F)F)=CC([C@@](NC(C2=CC=C(F)C(C(F)(F)F)=C2)=O)(CC3=CC=CC=C3)C4=CC=C(F)C(OC5CC5)=C4)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 67.15 | 100 | |
| ethanol | 67.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 671.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.49 mL | 7.45 mL | 14.89 mL |
| 5 mM | 0.3 mL | 1.49 mL | 2.98 mL |
| 10 mM | 0.15 mL | 0.74 mL | 1.49 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Qiao et al (2015) Triphenylethanamine derivatives as cholesteryl ester transfer protein inhibitors: discovery of N-[(1R)-1-(3-cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamid J.Med.Chem. 58 9010 PMID: 26524347
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Keywords: BMS 795311, BMS 795311 supplier, BMS795311, cholesteryl, ester, transfer, protein, CETP, potent, inhibitors, inhibits, orally, bioavailable, high, density, lipoprotein, cholesterol, HDL-C, Other, Transferases, Lipid, Metabolism, 5762, Tocris Bioscience
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