- Anacetrapib (MK-0859)
- Evacetrapib (LY2484595)
- Torcetrapib
| Dalcetrapib (JTT-705, RO4607381)rhCETP inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | Dalcetrapib is an inhibitor of rhCETP with IC50 value of 0.2 μM. | |||||
| Targets | rhCETP | |||||
| IC50 | 0.2 μM | |||||
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| Cas No. | 211513-37-0 | SDF | Download SDF |
| Chemical Name | S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate | ||
| Canonical SMILES | CCC(CC)CC1(CCCCC1)C(=O)NC2=CC=CC=C2SC(=O)C(C)C | ||
| Formula | C23H35NO2S | M.Wt | 389.59 |
| Solubility | ≥12.7 mg/mL in DMSO, ≥80.2 mg/mL in EtOH, <2.46 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 6 μM for CETP inhibition in human plasma
Cholesteryl ester transfer protein (CETP) is a plasma protein that transfers neutral lipids among the lipoproteins. Its most important action is the exchange of cholesteryl esters in high-density lipoprotein (HDL)for triglycerides in very low-density lipoprotein. Thus, CETP is a potentially atherogenic protein, and its atherogenicity has been supported by many studies. Dalcetrapib is a novel inhibitors of CETP.
In vitro: Dalcetrapib achieved 50% inhibition of CETP activity in human plasma at a concentration of 6 μM. The mechanism of action was considered to involve the formation of a disulfide bond between the thiol form of Dalcetrapib and the cysteine residue at position 13 (Cys13) of CETP. [1].
In vivo: Dalcetrapib achieved 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. It increased the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 or 100 mg/kg once a day for 3 days to male Japanese white rabbits [1].
Clinical trials: In a phase II study, Dalcetrapib showed no evidence of a pathological effect related to the arterial wall over 24 months. Moreover, this trial suggests possible beneficial vascular effects of dalcetrapib, including the reduction in total vessel enlargement over 24 months, but long-term safety and clinical outcomes efficacy of dalcetrapib need to be analysed [2].
References:[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 randomisedclinical trial. Lancet. 2011;378(9802):1547-59.
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大多数药物在体内都是和特异性受体相互作用，改变细胞的生理生化功能而产生效应。目前已经确定的受体有30多种，根据受体存在的标准，受体可大致分为三类：
1．细胞膜受体：位于靶细胞膜上，如胆碱受体、肾上腺素受体、多巴胺受体、阿片受体等。
2．胞浆受体：位于靶细胞的胞浆内，如肾上腺皮质激素受体、性激素受体。
3．胞核受体：位于靶细胞的细胞核内，如甲状腺素受体。
另外也可根据受体的蛋白结构、信息转导过程、效应性质、受体位置等特点将受体分为四类：
1．含离子通道的受体（离子带受体）：如N-型乙酰胆碱受体含钠离子通道。
2．G蛋白偶联受体：M-乙酰胆碱受体、肾上腺素受体等。
3．具有酪氨酸激酶活性的受体：如胰岛素受体。
4．调节基因表达的受体（核受体）：如甾体激素受体、甲状腺激素受体等。
有些受体具有亚型，各种受体都有特定的分布部位核特定的功能，有些细胞也有多种受体。
请教各位大神，我最近在做WB，565KD的蛋白，动物组织的样品，听说样品制备需要蔗糖裂解液，请问这个是必须的嘛？用一般蛋白提取方法制备可以吗？还有电泳和转膜条件能否分享一下。不胜感激
