化学信息：
| 化学名 | 5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide |
|
| 简称 | FIPI | |
| 别名 |
GTPL8781, SCHEMBL10311363, CTK8E9240, DTXSID60587488, SYN5173, BDBM123744 |
|
| 中文名 | N/A | |
| 化学式 | C23H24FN5O2 | |
| 分子量 | 421.47 | |
| CAS号 | 939055-18-2 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO15mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.19ml DMSO，或者每4.21mg加入1ml DMSO，配制成10mM溶液。SF1105-10mM用DMSO配制。 |
生物信息：
| 产品描述 | FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50=25nM) and PLD2 (IC50=20nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. | ||||
| 信号通路 | Others | ||||
| 靶点 | PLD1 | PLD2 | － | － | － |
| IC50 | 25nM | 20nM | － | － | － |
| 体外研究 | FIPI is a potent, concentration-dependent PLD2 inhibitor, and we show here that it inhibits PLD1 equally well under standard in vitro assay conditions. FIPI was added into the cell culture media 1 h before performing an in vivo PLD assay and was found to be a potent inhibitor of PLD2 with an IC50 of 10nM. The typical localization of PLD1 to peri-nuclear membrane vesicles and PLD2 to the plasma membrane were not affected by exposure to FIPI and and FIPI did not decrease PIP2 availability on the plasma membrane in PLD1- and PLD2-overexpressing cells as assessed using an enhanced GFP-fused PIP2 sensor. FIPI did not significantly inhibit p38 or ERK phosphorylation in bone marrow-derived macrophages stimulated with lipopolysaccharide. FIPI inhibition of PLD did diminish fmlP-directed chemotaxis(p<0.01), validating this role for PLD function and suggesting that PLD regulates chemotaxis via mechanisms distinct from affecting MAKP signaling. | ||||
| 体内研究 | N/A | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SF1105-10mM | FIPI (PLD1/2抑制剂) | 10mM×0.2ml |
| SF1105-5mg | FIPI (PLD1/2抑制剂) | 5mg |
| SF1105-25mg | FIPI (PLD1/2抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
