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939055-18-2

中文名称 FIPI
英文名称 FIPI
CAS 939055-18-2
分子式 C23H24FN5O2
分子量 421.47
MOL 文件 939055-18-2.mol
更新日期 2023/03/20 15:41:25
939055-18-2 结构式 939055-18-2 结构式

基本信息

中文别名
化合物FIPI
5-氟-2-吲哚基脱氯卤培米特
英文别名
FIPI
CS-1511
FIPI HYDROCHLORIDE
5-Fluoro-2-Indolyl des-Chlorohalopemide
5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide
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
所属类别
生物化工:激动剂抑制剂

物理化学性质

储存条件-20°C储存
溶解度DMSO : 14.67 mg/mL (34.81 mM; Need ultrasonic and warming)
形态粉末
FIPI价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-12807FIPI
FIPI
939055-18-25mg850元
2024/04/30HY-12807FIPI
FIPI
939055-18-210mM * 1mLin DMSO935元
2024/04/30S7321FIPI
FIPI
939055-18-25mg980.16元

常见问题列表

生物活性
FIPI (5-Fluoro-2-indolyl deschlorohalopemide) 是一种卤培米特 (halopemide)的衍生物,是一种有效且选择性的 phospholipase D 抑制剂,对 PLD1 和 PLD2 的IC50值分别为25 nM和20 nM。
靶点
TargetValue
PLD2
(Cell-free assay)
20 nM
PLD1
(Cell-free assay)
25 nM
体外研究

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.

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