FIPI

Catalog No.S7321 Batch:S732101

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Technical Data

Formula

C23H24FN5O2

Molecular Weight 421.47 CAS No. 939055-18-2
Solubility (25°C)* In vitro DMSO 45 mg/mL (106.76 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.75mg/ml Taking the 1 mL working solution as an example, add 50 μL of 15 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 45 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

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]

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]

Protocol (from reference)

Cell Assay:

[1]

  • 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.

Animal Study:

[2]

  • Animal Models

    6-10-week-old C57BL/6 mice, Pld1-/-/Pld2-/- mice

  • Dosages

    3 mg/kg

  • Administration

    IP

Selleck's FIPI has been cited by 1 publication

A light-controlled phospholipase C for imaging of lipid dynamics and controlling neural plasticity [ Cell Chem Biol, 2024, S2451-9456(24)00090-4] PubMed: 38582083

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.