FIPI
中文名称 | FIPI |
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中文同义词 | 5-氟-2-吲哚基脱氯卤培米特;化合物FIPI;FIPI游离;5-氟-N-(2-(4-(2-氧代-2,3-二氢-1H-苯并[D]咪唑-1-基)哌啶-1-基)乙基)-1H-吲哚-2-甲酰胺 |
英文名称 | FIPI |
英文同义词 | FIPI;FIPI HYDROCHLORIDE;5-Fluoro-2-Indolyl des-Chlorohalopemide;N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-5-fluoro-1H-indole-2-carboxamide;N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethy]-5-fluoro-1H-indole-2-carboxamide hydrochloride;CS-1511;5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide;1H-Indole-2-carboxamide, N-[2-[4-(2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-5-fluoro- |
CAS号 | 939055-18-2 |
分子式 | C23H24FN5O2 |
分子量 | 421.47 |
EINECS号 | |
相关类别 | 抑制剂 |
Mol文件 | 939055-18-2.mol |
结构式 |
FIPI 性质
密度 | 1.349±0.06 g/cm3(Predicted) |
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储存条件 | Store at -20°C |
溶解度 | DMSO:14.67 mg/mL(34.81 mM;需要超声波和加热) |
形态 | 粉末 |
酸度系数(pKa) | 12.04±0.30(Predicted) |
颜色 | 浅黄至卡其色 |
Target | Value |
PLD2
(Cell-free assay) | 20 nM |
PLD1
(Cell-free assay) | 25 nM |
Despite the high clearance of greater than 2 L/h/kg, FIPI shows a half-life of greater than 5 h, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%. FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM. FIPI is not an irreversible suicide inhibitor but neither is it rapidly and completely reverses upon removal of the drug. IPI does not alter PLD subcellular localization, access to PIP2, actin stress fibers, or upstream signaling events. FIPI rescues PLD2-suppressed membrane ruffling and cell spreading. FIPI attenuats the thimerosal-induced PLD activation, and the Hg-induced PLD activation in MAECs in a dose-dependent manner, and the agonist- and oxidant-induced PLD activation in a dose-dependent manner in MAECs.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-12807 | FIPI FIPI | 939055-18-2 | 5mg | 850元 |
2024/08/19 | HY-12807 | FIPI FIPI | 939055-18-2 | 10mM * 1mLin DMSO | 935元 |