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| 品牌 | absin | CAS | 875446-37-0 |
|---|---|---|---|
| 分子式 | C30H25F10NO3 | 纯度 | ＞98% |
| 分子量 | 637.51 | 货号 | abs810687 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent, selective | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Anacetrapib 875446-37-0
| 产品描述 | |
| 描述 | Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | MK-0859, MK 0859, MK0859 |
| 外观 | Powder |
| 可溶性/溶解性 | Ethanol ：117 mg/mL (183.5 mM) DMSO ：117 mg/mL (183.5 mM) |
| 生物活性 | |
| 靶点 | rhCETP,Mutant CETP (C13S) |
| In vitro(体外研究) | Anacetrapib is not only able to increase HDL-cholesterol, but also further decreases LDL-cholesterol when taken in combination with a statin. Anacetrapib dose-dependently and significantly decreases the transfer of CE from HDL3 to HDL2. Anacetrapib doesn't affect the amount of -dalcetrapibthiol bound to rhCETP. Anacetrapib decreases pre-β-HDL formation by more than 46%. Anacetrapib potently blocks CE and TG transfer in 95% human serum. |
| In vivo(体内研究) | In a dyslipidemic hamster model, 60 mg/kg/day Anacetrapib for 2 weeks results in a 94% reduction in CETP activity and 47% increase in HDL-cholesterol compared with control animals; non-HDL-cholesterol concentrations are not affected. In addition, Anacetrapib promotes reverse cholesterol transport from macrophages, and leads to a 30% increase in fecal cholesterol content. HDL from Anacetrapib-treated hamsters reveals an increase in SR-B1- and ABCG1-mediated efflux compared with controls. After oral administration of Anacetrapib at 10 mg/kg, ∼80 and 90% of the radioactive dose is recovered over 48 hous postdose from rats and monkeys, respectively. The majority of the administered radioactive dose is excreted unchanged in feces in both species. |
| 研究领域 | |
| 研究领域 | CancerCancer MetabolismMetabolic signaling pathwayMetabolism of lipids and lipoproteins CardiovascularAtherosclerosisLipid transport CardiovascularLipids / LipoproteinsLipid MetabolismCholesterol Metabolism MetabolismTypes of diseaseHeart disease MetabolismPathways and ProcessesMetabolic signaling pathwaysLipid and lipoprotein metabolismCholesterol Metabolism MetabolismPathways and ProcessesMetabolic signaling pathwaysLipid and lipoprotein metabolismLipid metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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