Evacetrapib (LY2484595)

製品コードS2925 バッチS292501

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C31H36F6N6O2
分子量 638.65 CAS No. 1186486-62-3
Solubility (25°C)* 体外 DMSO 12.8 mg/mL (20.04 mM)
Ethanol 12.8 mg/mL (20.04 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension
15% Captisol

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 10.000mg/ml (15.66mM) Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Evacetrapib (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.
in vitro Evacetrapib (LY2484595) inhibits human plasma CETP protein with IC50 of 26 nM. This compound (< 10 μM) does not induce aldosterone or cortisol synthesis in H295R cells. [1]
in vivo 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. This compound (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 this chemical in two dose-response studies are calculated to be 3.5 mg/kg and 4.1 mg/kg respectively. It (< 200 mg/kg) does not increase blood pressure in Zucker diabetic fatty rats. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
The medium contains 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℃. 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 receives 97.5 μL diluted CETP protein (final concentration 7 nM) and 2.5 μL of this compound stock. After a 30 min incubation at 37 ℃, 5 μL of substrate stock, 0.16 μL of VLDL stock (2.5 mg/mL) and 145 μL of CETP buffer are added, and the incubation is continued for another 4 hours. The fluorescent signal is measured in a fluorescent plate reader with 544 nm excitation and 595 nm emission upon the transfer of fluorescent cholesterol ester analogs to apoB-containing lipoproteins. IC50 values (concentration of this compound causing a 50% inhibition of CETP activity) are determined by nonlinear regression.
動物実験 動物モデル Human ApoAI and CETP double transgenic mice
投薬量 30 mg/kg
投与方法 Orally

参考

  • https://pubmed.ncbi.nlm.nih.gov/21957197/

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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