價格 | ¥213 | ¥483 | ¥818 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2025-02-28 |
中文名稱:化合物 Evacetrapib | 英文名稱:Evacetrapib |
CAS:1186486-62-3 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 98.53% | 產(chǎn)品類別: 抑制劑 |
貨號: T6262 |
名稱 | Evacetrapib |
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. |
激酶實驗 | 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]. |
體外活性 | 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] |
體內(nèi)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] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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) |
關鍵字 | inhibit | LY-2484595 | Inhibitor | Evacetrapib | LY 2484595 | CETP | Cholesteryl ester transfer protein |
相關產(chǎn)品 | Anacetrapib | Granotapide | Dalcetrapib | Obicetrapib | Lomitapide Mesylate | KD-026 | Lomitapide | Torcetrapib | Implitapide | TAP311 | BMS-212122 | Dirlotapide |
相關庫 | 抑制劑庫 | 脂代謝化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗心血管疾病化合物庫 | NO PAINS 化合物庫 | 抗肥胖化合物庫 | 臨床期小分子藥物庫 | 藥物功能重定位化合物庫 | 抗代謝疾病化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學,分子砌塊,生物技術服務 | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務 |
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