FIPI Phospholipase (e.g. PLA) inhibitor

Cat.No.S7321

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 Phospholipase (e.g. PLA) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 421.47

Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 421.47 Formula

C23H24FN5O2

Storage (From the date of receipt)
CAS No. 939055-18-2 -- Storage of Stock Solutions

Synonyms 5-Fluoro-2-indolyl deschlorohalopemide Smiles C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCNC(=O)C4=CC5=C(N4)C=CC(=C5)F

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
PLD2 [1]
(Cell-free assay)
20 nM
PLD1 [1]
(Cell-free assay)
25 nM
In vitro

FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM. This compound efficiently crosses cell membranes and inhibits PLD1 and PLD2 action on their endogenous substrate in the cytoplasmic environment.[1]

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, this compound-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]

References

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