生物活性 Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC50s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively[1][2].
体外研究(In Vitro) Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation[1]. Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner[3].
体内研究 (In Vivo) Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits[2]. Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol[1].
Animal Model: Male JW rabbits[2] Dosage: 30 or 100 mg/kg Administration: Oral administration, once a day for 3 days Result: Increased plasma HDL cholesterol by 27% and 54% at 30 mg/kg and 100 mg/kg, respectively.
分子量 389.59
性状 Solid
Formula C23H35NO2S
CAS 号 211513-37-0
中文名称 达塞曲匹
运输条件 Room temperature in continental US; may vary elsewhere.
储存方式 Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 溶解性数据 In Vitro: DMSO : ≥ 50 mg/mL (128.34 mM)
* "≥" means soluble, but saturation unknown.
配制储备液 浓度溶剂体积质量 1 mg 5 mg 10 mg 1 mM 2.5668 mL 12.8340 mL 25.6680 mL 5 mM 0.5134 mL 2.5668 mL 5.1336 mL 10 mM 0.2567 mL 1.2834 mL 2.5668 mL * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: