CAS NO: | 262352-17-0 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 600.47 |
Cas No. | 262352-17-0 |
Formula | C26H25F9N2O4 |
Solubility | ≥22.4 mg/mL in DMSO; insoluble in H2O; ≥69 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate |
Canonical SMILES | CCC1CC(C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C(=O)OC |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。 |
Torcetrapib是CETP的抑制剂,IC50值为37 nM,其作用是提升血浆中的HDL-C,降低非HDL-C。抑制胆固醇酯转移蛋白(CETP)对血浆脂蛋白水平有显著效果。
体外实验:在H295R细胞中,使用torcetrapib处理24或48小时后,剂量依赖性增加醛固酮释放,这种作用是通过钙通道介导的,钙通道阻滞剂完全阻断torcetrapib诱导的类皮质激素释放和钙升高。在H295R细胞系中,1 μM torcetrapib显著增加类固醇合成基因CYP11B2和CYP11B1的表达[1]。
在体实验:家兔喂食致动脉粥样饮食,其中torcetrapib的剂量可以将HDL-C的含量增加至少3倍,在整个研究期间,70%-80%的CETP活性被抑制。在两组中,非HDL-C含量均增加,但在研究结束后,没有明显的统计学差异[2]。
临床试验:Torcetrapib治疗增加死亡率和未知机制发病率的风险。虽然有证据表明这种风险是由于torcetrapib的脱靶效应,但不能排除是CETP抑制剂的副作用[3]。
参考文献:
[1] Hu X, Dietz JD, Xia C, Knight DR, Loging WT, Smith AH, Yuan H, Perry DA, Keiser J. Torcetrapib induces aldosterone and cortisol production by an intracellular calcium-mediated mechanism independently of cholesteryl ester transfer protein inhibition. Endocrinology. 2009;150(5):2211-9.
[2] Morehouse LA, Sugarman ED, Bourassa PA, Sand TM, Zimetti F, Gao F, Rothblat GH, Milici AJ. Inhibition of CETP activity by torcetrapib reduces susceptibility to diet-induced atherosclerosis in New Zealand White rabbits. J Lipid Res. 2007;48(6):1263-72.
[3] Barter PJ, Caulfield M, Eriksson M, Grundy SM, Kastelein JJ, Komajda M, Lopez-Sendon J, Mosca L, Tardif JC, Waters DD, Shear CL, Revkin JH, Buhr KA, Fisher MR, Tall AR, Brewer B; ILLUMINATE Investigators. Effects of torcetrapib in patients at high risk for coronary events. N Engl J Med. 2007;357(21):2109-22.
Description | Torcetrapib是胆固醇酯转移蛋白(CETP)的抑制剂,IC50值为50 nM。 | |||||
靶点 | CETP | |||||
IC50 | 50 nM |