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Evacetrapib is a benzazepine inhibitor of cholesteryl ester transfer protein (CETP; IC50s = 5.5 and 26 nM for human recombinant and plasma-derived proteins, respectively).{41797} It is selective for CETP over a panel of cell surface and nuclear receptors with no significant inhibition at 1 µM. Evacetrapib (1-10 µM) reduces expression of the serine protease proprotein convertase subtilisin kexin 9 (PCSK9) and the LDL receptor (LDLR) in HepG2 cells in a dose-dependent manner with no effect on cell viability.{41798} It also reduces protein levels of LDLR, SREBF2-M, and PCSK9 in HepG2 lysates, nuclear extracts, and culture medium, respectively, in a dose-dependent manner. Oral administration of evacetrapib (30 mg/kg) inhibits CETP activity by 98.5, 98.6, and 18.4% after four, eight, and 24 hours, respectively, in serum from transgenic mice expressing human CETP and ApoA1.{41797} Evacetrapib increases HDL cholesterol levels in CETP/ApoA1 transgenic mice in a dose-dependent manner, including by 129.7% eight hours following administration of a 30 mg/kg dose.
Territorial Availability: Available through Bertin Technologies only in France
| Size | 10 mg, 100 mg, 5 mg, 50 mg |
|---|---|
| Shipping | dry ice |
| CAS number | 1186486-62-3 |
| Molecular formula | C31H36F6N6O2 |
| Smiles | CN(N=N1)N=C1N([C@@H]2C(C=C(C)C=C3C)=C3N(C[C@@H]4CC[C@@H](C(O)=O)CC4)CCC2)CC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5 |
| Molecular weight | 638,7 |
| Custom code | 2902.90 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| UNSPSC code | 12352100 |
Cayman Chemical’s mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.
Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.
Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.
Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.
Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009
Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.
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