Evacetrapib (LY2484595)
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.
Evacetrapib是一种强效的胆固醇酯转移蛋白（CETP）选择性抑制剂，IC50值为5.5 nM[1]。
作为CETP的苯并氮杂基抑制剂，Evacetrapib可增加HDL胆固醇，用于冠状动脉疾病的治疗。Evacetrapib在体内外均有效。Evacetrapib在含人重组CETP的缓冲实验和含人血浆CETP的血浆实验中对CETP的IC50值分别为5.5 nM和26 nM。在人CETP/ApoAI双转基因小鼠系动物模型中，30 mg/kg的Evacetrapib口服给药后显著抑制CETP活性以及提升HDL水平。此外，Evacetrapib的ED50值小于5mg/kg。相比以前的CETP抑制剂，Evacetrapib具有较少的副作用。据发现，它不能增加Zucker糖尿病肥胖大鼠的血压，也不能诱导H295R细胞合成醛固酮或皮质甾醇[1]。
参考文献：
[1] Cao G, Beyer TP, Zhang Y, Schmidt RJ, Chen YQ, Cockerham SL, Zimmerman KM, Karathanasis SK, Cannady EA, Fields T, Mantlo NB. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J Lipid Res. 2011 Dec; 52(12):2169-76.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 638.65 |
| Cas No. | 1186486-62-3 |
| Formula | C31H36F6N6O2 |
| Solubility | ≥32.1 mg/mL in DMSO; insoluble in H2O; ≥50.4 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-[[(5S)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C2C(=C1)C(CCCN2CC3CCC(CC3)C(=O)O)N(CC4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C5=NN(N=N5)C)C |
| 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。 |
| 描述 | Evacetrapib是一种强效的胆固醇酯转移蛋白（CETP）选择性抑制剂，IC50值为5.5 nM。 | |||||
| 靶点 | CETP | |||||
| IC50 | 5.5 nM | |||||
质量控制和MSDS
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化学结构
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