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| Size | Price | Stock |
|---|---|---|
| 5mg | $120 | 3-6 Days |
| 10mg | $180 | 3-6 Days |
| 25mg | $279 | 3-6 Days |
| 50mg | $415 | 3-6 Days |
| 100mg | $619 | 3-6 Days |
| 250mg | $1080 | 3-6 Days |
| 500mg | $1550 | 3-6 Days |
: Cat #: V3177 CAS #: 1781834-93-2 Purity ≥ 98%
Description: FIPI HCl, the hydrochloride salt of FIPI which is formerly known as 5-Fluoro-2-indolyl deschlorohalopemide, is a derivative of halopemide which potently and selectively inhibits both PLD1 (phospholipase D) and PLD2 with IC50 values of 25 nM and 20 nM, respectively. FIPI is able to attenuate mercury-induced lipid signaling resulting in protection against cytotoxicity in aortic endothelial cells. FIPI rapidly blocks in vivo PA production with low nanomolar potency. FIPI has favorable pharmacokinetics with a half-life of greater than 5 hours, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%. FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner with 50% loss of activity observed at approximately 25 nM.
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| Molecular Weight (MW) | 457.93 |
|---|---|
| Molecular Formula | C23H25ClFN5O2 |
| CAS No. | 1781834-93-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: >10mM |
| Water: NA | |
| Ethanol: NA | |
| SMILES Code | O=C(C(N1)=CC2=C1C=CC(F)=C2)NCCN3CCC(N4C5=CC=CC=C5NC4=O)CC3.[H]Cl |
| Synonyms | FIPI HCl; 5-Fluoro-2-indolyl deschlorohalopemide |
| Protocol | In Vitro | In vitro activity: FIPI shows a half-life of greater than 5 h, a Cmax of greater than 10-fold the 50 versus PLD2, and moderate bioavailability of 18%.FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner, with 50% loss of activity observed at approximately 25 nM.FIPI attenuats the thimerosal-induced PLD activation, and the Hg-induced PLD activation in MAECs in a dose-dependent manner, and the agonist- and oxidant-induced PLD activation in a dose-dependent manner in MAECs. Kinase Assay: Phospholipase D activity is quantified using our established method of measuring the formation of [32P]-radiolabeled PBt. Cellular lipids are extracted and PBt is isolated using our published methods of lipid extraction and thin layer chromatographic separation, respectively. Radioactivity is measured using liquid scintillation counting and quantified as DPM normalized to 106 counts in the total cellular lipid extract or as percentage of control (vehicle-treated cells). Cell Assay: Cytotoxicity in MAECs is determined by assaying the extent of reduction in MTT in intact cells using the commercial MTT reduction assay kit. At the end of the experimental treatments, MTT solution (10% vol/vol in MEM) is added and the cells are incubated for 3 hours, following which MTT solvent is added in an amount equal to the original culture volume. Absorbance of the reduced MTT is determined spectrophotometrically, according to the manufacturer's recommendations. |
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| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1837 mL | 10.9187 mL | 21.8374 mL | 43.6748 mL |
| 5mM | 0.4367 mL | 2.1837 mL | 4.3675 mL | 8.7350 mL |
| 10mM | 0.2184 mL | 1.0919 mL | 2.1837 mL | 4.3675 mL |
| 20mM | 0.1092 mL | 0.5459 mL | 1.0919 mL | 2.1837 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.