Torcetrapib
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.
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.
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 |
SDF | Download SDF |
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 | 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 | 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 |
质量控制和MSDS
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