Anacetrapib (MK-0859)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Anacetrapib，也称为MK-0859，是一种有效的和选择性的胆固醇酯转运蛋白(CETP)抑制剂，强烈抑制CETP介导的胆固醇酯和甘油酸三脂转运，IC50值分别为16 nM和29 nM。Anacetrapib主要经CYP3A4代谢，通过对联苯基部分的氧去甲基化和羟基化，以及对异丙基侧链的羟基化，分别形成三个氧化代谢产物M1、M2和M3。由于Anacetrapib可强效降低低密度脂蛋白(LDL)胆固醇水平和增加高密度脂蛋白(HDL)胆固醇水平，且无任何副作用，目前被用来治疗原发性高胆固醇血症和混合性高脂血症[1]。
参考文献：
[1]. 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.
[2]. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 637.51 |
| Cas No. | 875446-37-0 |
| Formula | C30H25F10NO3 |
| Synonyms | MK 0859, MK0859 |
| Solubility | ≥31.9 mg/mL in DMSO; insoluble in H2O; ≥86.6 mg/mL in EtOH |
| Chemical Name | (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one |
| SDF | Download SDF |
| Canonical SMILES | CC1C(OC(=O)N1CC2=C(C=CC(=C2)C(F)(F)F)C3=CC(=C(C=C3OC)F)C(C)C)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | Anacetrapib是一种有效的、选择性的和可逆的rhCETP和突变 CETP(C13S)抑制剂，IC50值分别为7.9 nM和11.8 nM。 | |||||
| 靶点 | rhCETP | mutant CETP(C13S) | ||||
| IC50 | 7.9 nM | 11.8 nM | ||||
质量控制和MSDS
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化学结构
相关生物数据
