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Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。
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Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 213 | 现货 | |
5 mg | ¥ 483 | 现货 | |
10 mg | ¥ 818 | 现货 | |
25 mg | ¥ 1,820 | 现货 | |
50 mg | ¥ 3,130 | 现货 | |
100 mg | ¥ 4,480 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 678 | 现货 |
产品描述 | Evacetrapib (LY2484595) (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3. |
靶点活性 | CETP:5.5 nM |
体外活性 | Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. Evacetrapib (LY2484595) (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. [1] |
体内活性 | Evacetrapib (LY2484595) (30 mg/kg, orally) results in 98.4%, 98.6%, and 18.4% inhibition of CETP activity at 4 hours, 8 hours and 24 hours post dose respectively in human ApoAI and CETP double transgenic mice. Evacetrapib (LY2484595) (30 mg/kg) results in 129.7% increase in HDL-C 8 hours after oral administration. The ED50 values of CETP inhibitory activity 8 hours post oral dosing for Evacetrapib (LY2484595) in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. Evacetrapib (LY2484595) (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. [1] |
激酶实验 | Human CETP cDNA is amplified from a human liver cDNA library and the sequence is confirmed to be identical to the published sequence. The cDNA is subcloned into a pcDNA3.1 vector, under the control of CMV promoter. A stable line is established in CV1 cells in which the above-mentioned construct is used to express the recombinant human CETP. The medium contained the secreted recombinant CETP protein and the amount (19 ng/μL) is quantified by an ELISA kit. The medium is then aliquoted in 0.2% BSA and stored at -80°C. The stock CETP protein is diluted 150-fold in CETP buffer (10 mM Tris, 150 mM NaCl, and 2 mM EDTA) before use. The assay is set up in a 96-well plate. Each well received 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of compound stock. After a 30 min incubation at 37°C, 5 μL of substrate stock (the same stock used in the human plasma CETP assay), 0.16 μL of VLDL stock (2.5 mg/mL, Intracel) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 h. Signal is read for the human plasma CETP assay[1]. |
别名 | LY2484595 |
分子量 | 638.65 |
分子式 | C31H36F6N6O2 |
CAS No. | 1186486-62-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 13 mg/mL (20.4 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 11 mg/mL (17.2 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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