Home Metabolism Phospholipase (e.g. PLA) inhibitor FIPI For research use only.

FIPI

Synonyms: 5-Fluoro-2-indolyl deschlorohalopemide

FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively.

FIPI Chemical Structure

FIPI Chemical Structure

CAS No. 939055-18-2

Purity & Quality Control

Batch: S732101 DMSO]45 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.84%
99.84

FIPI Related Products

Signaling Pathway

Phospholipase (e.g. PLA) Signaling Pathways

Phospholipase (e.g. PLA) Signaling Pathway

Biological Activity

Description FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively.
Targets
PLD2 [1]
(Cell-free assay)		 PLD1 [1]
(Cell-free assay)
20 nM 25 nM
In vitro
In vitro

FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM. FIPI efficiently crosses cell membranes and inhibits PLD1 and PLD2 action on their endogenous substrate in the cytoplasmic environment.[1]
Cell Research Cell lines CHO cell lines, NIH3T3, macrophages, Min6 cells
Concentrations 7.5 nM, 25 nM, 75 nM, 250 nM, 750 nM
Incubation Time 5 min, 10 min, 15 min, 30 min, 60 min
Method

For the time-course study, cells are preincubated with 100 nM FIPI for 5, 10, 15, or 30 min followed by a 10-min incubation with 0.3% 1-butanol. For recovery experiments, cells are incubated with 2 μCi/ml[3H]palmitic acid and then switched to fresh growth medium containing 50 μg/ml cycloheximide. Thirty minutes later, one set of cells is treated with 100 nM FIPI for 30 min followed by three washes with PBS and addition of fresh growth medium containing cycloheximide. The cells are incubated for 1 or 8 h. During the last 30 min, FIPI is added to a second set of cells, after which all of the sets of cells are assayed for PLD activity.
In Vivo
In vivo

Mice that receives FIPI at a dose of 3 mg/kg displayes reduced occlusive thrombus formation upon chemical injury of carotid arteries or mesenterial arterioles. Similarly, FIPI-treated mice has smaller infarct sizes and significantly better motor and neurological function 24 hours after transient middle cerebral artery occlusion. This protective effect is not associated with major intracerebral hemorrhage or prolonged tail bleeding times.[2]
Animal Research Animal Models 6-10-week-old C57BL/6 mice, Pld1-/-/Pld2-/- mice
Dosages 3 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 421.47 Formula

C23H24FN5O2
CAS No. 939055-18-2 SDF --
Smiles C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCNC(=O)C4=CC5=C(N4)C=CC(=C5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (106.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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