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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Metabolism>CETP inhibitors>Anacetrapib
Anacetrapib
  • Anacetrapib
  • Anacetrapib
  • Anacetrapib
  • Anacetrapib
  • Anacetrapib

Anacetrapib NEW

Price Get Latest Price
Package 25KG
Min. Order: 1KG
Supply Ability: 50000KG/month
Update Time: 2023-10-12

Product Details

Product Name: Anacetrapib CAS No.: 875446-37-0
EC-No.: 1312995-182-4 Min. Order: 1KG
Purity: 99% Supply Ability: 50000KG/month
Release date: 2023/10/12

CAS:875446-37-0
MF:C30H25F10NO3
MW:637.51
EINECS:1312995-182-4
Product Categories:Inhibitor;CETP inhibitor;Aromatics;Chiral Reagents;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Anacetrapib
Mol File:875446-37-0.mol
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Anacetrapib Chemical Properties
Boiling point 555.3±50.0 °C(Predicted)
density 1.345
storage temp. Store at -20°C
solubility ≥31.9 mg/mL in DMSO; insoluble in H2O; ≥86.6 mg/mL in EtOH
form solid
pka-2.30±0.60(Predicted)
Anacetrapib Usage And Synthesis
UsesAn orally active and potent cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis, in particular dyslipidemia.
Biological Activityanacetrapib, also known as mk-0859, is a potent and selective inhibitor of cholesteryl ester transfer protein (cetp) that exhibits strong inhibition against cetp-mediated transfer of cholesteryl esters and triglycerides with values of inhibition constant ic50 of 16 nm and 29 nm respectively. anacetrapib is mainly metabolized by cyp3a4 through o-demethylation, hydroxylation on the biphenyl moiety and hydroxylation on the isopropyl side chain resulting in three oxidative metabolites m1, m2 and m3 respectively. anacetrapib is being investigated for the treatment of primary hypercholesterolemia and mixed hyperlipidemia due to its impressive effects to lower low-density lipoprotein (ldl) cholesterol levels and increase high-density lipoprotein (hdl) cholesterol levels without any associated major adverse events.tan ey, hartmann g, chen q, pereira a, bradley s, doss g, zhang as, ho jz, braun mp, dean dc, tang w, kumar s. pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys. drug metab dispos. 2010;38(3):459-473.kumar s, tan ey, hartmann g, biddle z, bergman aj, dru j, ho jz, jones an, staskiewicz sj, braun mp, karanam b, dean dc, gendrano in, graves mw, wagner ja, krishna r. metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans. drug metab dispos. 2010;38(3):474-483
Enzyme inhibitorThis cholesteryl ester transfer protein (or CETP) inhibitor (FW = 637.51 g/mol; CAS 875446-37-0), also known by the code name MK-0859, reduces plasma cholesterol concentrations, thereby increasing serum highdensity lipoprotein levels and preventing cardiovascular disease associated with hypercholesteremia. X-ray crystal studies suggest that CETP is a crescent-shaped protein with a 6-nm hydrophobic tunnel traversing its core Both of the tunnel’s two entrances face the protein’s concave surface, which most likely is the interaction platform for binding HDL particles and engaging its lipoprotein constituents. CETP mediates the reciprocal transfer of neutral lipids (e.g., cholesteryl esters and triglycerides) and phospholipids between different lipoprotein fractions in blood plasma. Anacetrapib is unlike many CETP inhibitors, which increase systolic blood pressure. Anacetrapib also exhibits a low-to-moderate degree of absorption after oral dosing and majority of the absorbed dose is eliminated via oxidation to a series of hydroxylated metabolites that undergo conjugation with glucuronate before excretion into bile. Unlike torcetrapib, another CETP inhibitor, anacetrapib does not elevate blood pressure, alter electrolytes, or cause any significant side effects.
targetrhCETP

Packing &shipping&Payment

Packing:25kg/drum
Shipping:by sea or by air
Payment:T/T,western union,moneygram
Packaging Details drum
Port:Tianjin
Lead Time :
Quantity(Kilograms)1 - 10000>10000
Est. Time(days)5To be negotiated

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Article illustrationCompany information
Hebei Mojin Biotechnology Co., Ltd, Our company is a professional in 4'-Methylacetophenone,Levamisole hydrochloride ,N-Methylformamide and other chemical reagents research and development production enterprises. Our business covers more than 30 countries, most of the big customers come from Europe, America and other countries in the world, we can guarantee the quality and price. In recent decades, with the efforts of all employees, we have established many cooperative companies in shandong, henan, guangdong and other places. Our corporate purpose is based on the market, enhance the strength, take the road of scientific and environmental sustainable development, relying on the country. Technology r & d center, increase the investment in r & d, based on the domestic market, expand the international market, manufacturing quality products, sincere service to the society, into a modern, ecological, scientific and technological enterprise world.

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