Powder: -20°C for 3 years | In solvent: -80°C for 1 year
XEN445 是一种内皮脂肪酶抑制剂(IC50:0.237 uM),具有显著的ADME 和PK 活性,可以增强小鼠血浆中高密度脂蛋白胆固醇浓度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 219 | 现货 | ||
2 mg | ¥ 318 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 3,670 | 现货 | ||
100 mg | ¥ 5,290 | 现货 | ||
500 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 638 | 现货 |
产品描述 | XEN445, a potent and selective endothelial lipase(EL) inhibitor (IC50=0.237 uM), exhibitis good ADME and PK properties. |
靶点活性 | endothelial lipase:0.237 μM |
体外活性 | XEN445 exhibits good specificity over LPL and HL, and great inhibition activity against EL. |
激酶实验 | In vitro PI3K lipid kinase assay: (1) For PI3Kγ: human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 μM ATP/100 nCi γ[33P]ATP, final concentrations) and lipid vesicles containing 18 μM PtdIns and 250 μM of PtdSer (final concentrations), in the presence of AS-605240 or DMSO. Kinase reaction is stopped by adding 250 μg of Neomycin-coated Scintillation Proximity Assay (SPA) beads. (2) For PI3Kα, β, and δ: varying amounts of ATP are incubated with the different purified PI3K isoforms and saturating concentrations of PtdIns. Consequently, IC50 determinations with PI3Kα, β, and δ, to evaluate inhibitor selectivity are performed as follows: 60 ng of PI3Kα are incubated at RT with kinase buffer, as described for PI3Kγ (but containing 89 μM ATP/300 nCi γ[33P]ATP and no Na Cholate, instead) and lipid vesicles containing 212 μM PtdIns and 58 μM of PtdSer. 100 ng of PI3Kβ are incubated at RT with kinase buffer (containing 70 μM ATP/300 nCi γ[33P]ATP, 4 mM MgCl2 and no Na Cholate) and lipid vesicles containing 225 μM PtdIns and 45 μM of PtdSer. 90 ng of PI3Kδ are incubated with kinase buffer (containing 65 μM ATP/300 nCi γ[33P]ATP, 1 mM MgCl2, and no Na Cholate) and lipid vesicles containing 100 μM PtdIns and 170 μM of PtdSer. The reactions are stopped after 2 hours. |
别名 | XEN 445, XEN-445, 2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸 |
分子量 | 366.33 |
分子式 | C18H17F3N2O3 |
CAS No. | 1515856-92-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 36.6 mg/mL (100 mM)
DMSO: 36.6 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.7298 mL | 13.6489 mL | 27.2978 mL | 68.2445 mL |
5 mM | 0.546 mL | 2.7298 mL | 5.4596 mL | 13.6489 mL | |
10 mM | 0.273 mL | 1.3649 mL | 2.7298 mL | 6.8244 mL | |
20 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4122 mL | |
50 mM | 0.0546 mL | 0.273 mL | 0.546 mL | 1.3649 mL | |
100 mM | 0.0273 mL | 0.1365 mL | 0.273 mL | 0.6824 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
XEN445 1515856-92-4 Metabolism Lipase Inhibitor inhibit XEN 445 XEN-445 2-[(3S)-3-(2-吡啶基甲氧基)-1-吡咯烷基]-5-(三氟甲基)苯甲酸 inhibitor