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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。
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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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 262 | 现货 | |
2 mg | ¥ 369 | 现货 | |
5 mg | ¥ 529 | 现货 | |
10 mg | ¥ 859 | 现货 | |
25 mg | ¥ 1,650 | 现货 | |
50 mg | ¥ 2,650 | 现货 | |
100 mg | ¥ 3,960 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 582 | 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 (mouse):2.8 nM, sEH (human):3.7 nM |
体内活性 | TPPU及两种4-(环己氧基)苯甲酸尿素sEHIs在以0.3 mg·kg(-1)口服剂量下,展现出高于10倍IC(50)的血浆浓度。尽管4-(环己氧基)苯甲酸尿素对猴子sEH的效力优于吡啶基尿素(TPAU和TPPU),但后者显示出更高的血浆浓度和更显著的药物样性质。TPPU和TPAU的最大血浆浓度(C(max))分别随剂量从0.3 mg·kg(-1)增至3 mg·kg(-1)和从0.1 mg·kg(-1)增至3 mg·kg(-1),尽管在这一剂量范围内并非线性增加。作为靶向作用的指标,TPPU治疗时亚油酸环氧化物与二醇的比率有所增加[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 |
Smiles | CCC(=O)N1CCC(CC1)NC(=O)Nc1ccc(OC(F)(F)F)cc1 |
密度 | 1.31 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 28 mg/mL (77.92 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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