化合物Evacetrapib T6262

Product Introduction
Bioactivity


英文名: Evacetrapib

描述: 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。

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].

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 13 mg/mL (20.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 11 mg/mL (17.2 mM)


关键字: inhibit | LY-2484595 | Inhibitor | Evacetrapib | LY 2484595 | CETP | Cholesteryl ester transfer protein

相关产品: TAP311 | Anacetrapib | Granotapide | CP-532623 | Implitapide | Obicetrapib | NAMI-A | Lomitapide | BMS-212122 | Lomitapide Mesylate

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Human Metabolite Library | Inhibitor Library | Anti-Obesity Compound Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Anti-Cardiovascular Disease Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途