| 产品编号 |
产品名称 |
产品包装 |
产品价格 |
| SF1105-10mM |
FIPI (PLD1/2抑制剂) |
10mM |
111.00元 |
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
|
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剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Monovich L, et al. Bioorg Med Chem Lett. 2007 Apr 15, 17(8), 2310-1.
2. Su W, et al. 5-Fluoro-2-indolyl des-chlorohalopemide (FIPI), a phospholipase D pharmacological inhibitor that alters cell spreading and inhibits chemotaxis. Mol Pharmacol. 2009 Mar;75(3):437-46.
包装清单：
|
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。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。