Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TPPU 是一种可溶性环氧化物水解酶(sEH)抑制剂,对猴子和人类的IC50分别为37和3.7 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 262 | 现货 | ||
5 mg | ¥ 597 | 现货 | ||
10 mg | ¥ 947 | 现货 | ||
25 mg | ¥ 1,830 | 现货 | ||
50 mg | ¥ 2,730 | 现货 | ||
100 mg | ¥ 3,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 688 | 现货 |
产品描述 | TPPU is a potent inhibitor of both human and mouse sEH (IC50 of 3.7 and 2.8 nM, respectively) |
靶点活性 | sEH (human):3.7 nM , sEH (mouse):2.8 nM |
体内活性 | TPPU and two 4-(cyclohexyloxy) benzoic acid urea sEHIs displayed high plasma concentrations (>10 × IC(50)), when dosed orally at 0.3 mg·kg(-1). Although the 4-(cyclohexyloxy) benzoic acid ureas were more potent against monkey sEH than piperidyl ureas (TPAU and TPPU), the latter compounds showed higher plasma concentrations and more drug-like properties. The C(max) increased with dose from 0.3 to 3 mg·kg(-1) for TPPU and from 0.1 to 3 mg·kg(-1) for TPAU, although it was not linear over this range of doses. As an indication of target engagement, ratios of linoleate epoxides to diols increased with TPPU administration[1]. |
动物实验 | PK parameters of 11 sEHIs in cynomolgus monkeys were determined after oral dosing with 0.3 mg/kg. Their physical properties and inhibitory potency in hepatic cytosol of cynomolgus monkeys were examined. Dose-dependent effects of the two inhibitors 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) and the related acetyl piperidine derivative, 1-trifluoromethoxyphenyl-3-(1-acetylpiperidin-4-yl) urea (TPAU), on natural blood eicosanoids[1] |
分子量 | 359.34 |
分子式 | C16H20F3N3O3 |
CAS No. | 1222780-33-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 28 mg/mL (77.92 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7829 mL | 13.9144 mL | 27.8288 mL | 69.572 mL |
5 mM | 0.5566 mL | 2.7829 mL | 5.5658 mL | 13.9144 mL | |
10 mM | 0.2783 mL | 1.3914 mL | 2.7829 mL | 6.9572 mL | |
20 mM | 0.1391 mL | 0.6957 mL | 1.3914 mL | 3.4786 mL | |
50 mM | 0.0557 mL | 0.2783 mL | 0.5566 mL | 1.3914 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。
TPPU 1222780-33-7 Metabolism Epoxide Hydrolase inhibit Inhibitor inhibitor