Dalcetrapib (JTT-705, RO4607381)
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.
IC50:人血浆中对CETP的抑制为6 μM
胆固醇酯转移蛋白(CETP)是一种血浆蛋白,参与传送脂蛋白中的中性脂质,它最重要的作用是交换高密度脂蛋白(HDL)中的胆固醇酯与极低密度脂蛋白中的甘油三酯。因此,CETP是一种潜在的致动脉粥样硬化蛋白,许多研究表明它的致动脉粥样硬化作用。Dalcetrapib是一种新型的CETP抑制剂。
体外实验:6 μM的dalcetrapib抑制人血浆中50%的CETP的活性,其作用机制可能是dalcetrapib的硫醇形式和CETP第13位半胱氨酸残基(Cys13)形成二硫键[1]。
在体实验:雄性日本白兔口服30 mg/kg剂量的dalcetrapib,对CETP活性抑制达到95%,雄性日本白兔每天一次口服剂量为30或100 mg/kg的dalcetrapib,连续服用3天,将血浆HDL胆固醇水平分别增加了27%和54%[1]。
临床试验:II期临床研究表明,超过24个月后,Dalcetrapib没有产生与动脉壁相关的明显的病理学效果。此外,该试验表明,dalcetrapib可能有利血管作用,超过24个月后,总血管扩张减少,其长期的安全性和临床疗效有待于进一步分析[2]。
参考文献:
[1] Shinkai H, Maeda K, Yamasaki T, Okamoto H, Uchida I. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. J Med Chem. 2000;43(19):3566-72.
[2] Fayad ZA, Mani V, Woodward M, Kallend D, Abt M, Burgess T, Fuster V, Ballantyne CM, Stein EA, Tardif JC, Rudd JH, Farkouh ME, Tawakol A. Safety and efficacy of dalcetrapib on atherosclerotic disease using novel non-invasive multimodality imaging (dal-PLAQUE): a randomised clinical trial. Lancet. 2011;378(9802):1547-59.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 389.59 |
Cas No. | 211513-37-0 |
Formula | C23H35NO2S |
Solubility | insoluble in H2O; ≥12.7 mg/mL in DMSO; ≥80.2 mg/mL in EtOH |
Chemical Name | S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate |
SDF | Download SDF |
Canonical SMILES | CCC(CC)CC1(CCCCC1)C(=O)NC2=CC=CC=C2SC(=O)C(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。 |
Description | Dalcetrapib是rhCETP的抑制剂,IC50值为0.2 μM。 | |||||
靶点 | rhCETP | |||||
IC50 | 0.2 μM |