化学信息：
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化学名
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5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide
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简称
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FIPI
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别名
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GTPL8781, SCHEMBL10311363, CTK8E9240, DTXSID60587488, SYN5173, BDBM123744
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中文名
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N/A
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化学式
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C23H24FN5O2
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分子量
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421.47
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CAS号
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939055-18-2
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO15mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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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.
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信号通路
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Others
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靶点
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PLD1
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PLD2
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－
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－
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－
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IC50
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25nM
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20nM
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－
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－
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－
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体外研究
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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.
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体内研究
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N/A
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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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：
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产品编号
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产品名称
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包装
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SF1105-10mM
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FIPI (PLD1/2抑制剂)
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10mM×0.2ml
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SF1105-5mg
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FIPI (PLD1/2抑制剂)
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5mg
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SF1105-25mg
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FIPI (PLD1/2抑制剂)
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25mg
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—
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说明书
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1份
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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。
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