TP0472993是一种口服有效的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双抑制剂,IC50 值分别为 140 nM 和 40 nM,适用于肾脏疾病的研究。
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描述 | CYP4A11/CYP4F2-IN-2 acts as a potent, orally available inhibitor that targets both cytochrome P450 4A11 and CYP4F2 enzymes, displaying IC50 values of 140 nM and 40 nM, respectively. This dual inhibitor holds promise for studies related to kidney diseases[1]. |
体内研究 | Administered orally in a single dose ranging from 0.03 to 1 mg/kg, CYP4A11/CYP4F2-IN-2 proportionally decreases the production of 20-HETE in the kidneys of rats[1]. When given intravenously at 0.5 mg/kg to mice, CYP4A11/CYP4F2-IN-2 shows a low clearance rate (1430 mL/h/kg), a moderate volume of distribution at steady state (763 mL/kg), and a short half-life (0.424 hours)[1]. At a dosage of 1 mg/kg administered intravenously to Sprague-Dawley (SD) rats, the inhibitor demonstrates a low clearance rate (226 mL/h/kg), a moderate volume of distribution at steady state (839 mL/kg), and a half-life of approximately 3.01 hours[1]. Following oral administration at 1 mg/kg to SD rats, CYP4A11/CYP4F2-IN-2 reaches a maximum concentration (Cmax) of 623 ng/mL, has a half-life of 3.03 hours, and exhibits high bioavailability (97.7%)[1]. |
体外研究 | CYP4A11/CYP4F2-IN-2 effectively reduces the production of 20-Hydroxyeicosatetraenoic acid (20-HETE) from arachidonic acid within human kidney microsomes, showing an IC50 value of 29 nM[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.33mL 0.67mL 0.33mL |
16.65mL 3.33mL 1.66mL |
33.29mL 6.66mL 3.33mL |
CAS号 | 2126874-77-7 |
分子式 | C16H20N4O2 |
分子量 | 300.356 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 25 mg/mL(83.23 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |