| 中文名称 |
Dalcetrapib
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| 中文别名 |
达塞曲匹;CETP抑制剂;Dalcetrapib (JTT-705, RO4607381) 抑制剂;达塞曲匹标准品;CETP 抑制剂
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| 英文名称 |
Dalcetrapib
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| 英文别名 |
Propanethioic acid,2-methyl-, S-[2-[[[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino]phenyl] ester;Dalcetrapib;CETP inhibitors;Dalcetrapib (JTT-705, RO4607381);Dalcetrapib(JTT-705,JTT705,RO4607381);JTT705;JTT-705;S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate;RO 4607381;RO-4607381;Unii-3D050liq3h;S-[2-[[1-(2-ethylbutyl)cyclohexane]carbonylamino]phenyl]-2-methylpropanethioate;2-Methylpropanethioic acid S-[2-[1-(2-ethylbutyl)cyclohexylcarboxamido]phenyl] ester;JTT 705;RO4607381;3D050LIQ3H;AK185456;S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate;PubChem22426;Tube711;Dalcetrapib (USAN/I
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| Cas No. |
211513-37-0
|
| 分子式 |
C23H35NO2S
|
| 分子量 |
389.59
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
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| 详情描述 |
Dalcetrapib (JTT-705) 是一种具有口服活性的胆固醇酯转运蛋白 (CETP) 抑制剂,对 rhCETP 和人血浆 CETP 的 IC50 分别为 204.6 nM 和 6 μM。
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| 产品详情 |
Dalcetrapib (JTT-705) 是一种具有口服活性的胆固醇酯转运蛋白 (CETP) 抑制剂,对 rhCETP 和人血浆 CETP 的 IC50 分别为 204.6 nM 和 6 μM。
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| 生物活性 |
Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC 50 s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 204.6 nM (rhCETP), 6 μM (human plasma CETP)
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| 体外研究(In Vitro) |
Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation.Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 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.
Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
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| ClinicalTrial |
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| 参考文献 |
[1]. Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.[2]. Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572.
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| 溶解度数据 |
In Vitro: DMSO : ≥ 50 mg/mL (128.34 mM)配制储备液
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[1]. Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.[2]. Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。