Torcetrapib

A CETP inhibitor

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库存: 现货

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5mg

￥650.00

520.00

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10mg

￥862.00

690.00

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50mg

￥3437.00

2750.00

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货号: ajci15938
CAS: 262352-17-0
别名: 托彻普; CP-529414
分子式: C26H25F9N2O4
分子量: 600.47
纯度: >98%
溶解度: ≥ 22.4 mg/mL in DMSO, ≥ 69 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

Torcetrapib is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma. Inhibition of cholesteryl ester transfer protein (CETP) has been shown to have a substantial effect on plasma lipoprotein levels.

In vitro: Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment, this effect is mediated by calcium channel as calcium channel blockers completely blocks torcetrapib-induced corticoid release and calcium increase. Torcetrapib (1 μM) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines [1].

In vivo: Researchers tested torcetrapib in rabbits fed an atherogenic diet at a dose sufficient to increase HDL-C by at least 3-fold. CETP activity was inhibited by 70–80% throughout the study. Non-HDL-C increased in both groups, but there was no difference apparent by the study’s end [2].

Clinical trial: Torcetrapib therapy resulted in an increased risk of mortality and morbidity of unknown

mechanism. Although there was evidence of an off-target effect of torcetrapib, adverse effects related to CETP inhibition cannot be ruled out [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.