Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TPPU is a potent inhibitor of both human and mouse sEH (IC50 of 3.7 and 2.8 nM, respectively)
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 7,500 | |||
5 mg | 在庫あり | ¥ 15,500 | |||
10 mg | 在庫あり | ¥ 27,000 | |||
25 mg | 在庫あり | ¥ 54,500 | |||
50 mg | 在庫あり | ¥ 89,500 | |||
100 mg | 在庫あり | ¥ 130,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 17,000 |
説明 | TPPU is a potent inhibitor of both human and mouse sEH (IC50 of 3.7 and 2.8 nM, respectively) |
ターゲット&IC50 | sEH (human):3.7 nM , sEH (mouse):2.8 nM |
In vivo | 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]. |
動物実験 | 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)
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TPPU 1222780-33-7 Metabolism Epoxide Hydrolase inhibit Inhibitor inhibitor