| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
FIPI HCl targets phospholipase D (PLD), specifically inhibiting both PLD1 and PLD2 isoforms. PLD catalyzes the hydrolysis of phosphatidylcholine to form phosphatidic acid (PA), which is essential for many biological processes including Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking.
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| ln Vitro |
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 manufacturers recommendations. In vitro, FIPI inhibits both PLD1 and PLD2 in a dose-dependent manner with 50% loss of activity observed at approximately 25 nM. It attenuates thimerosal-induced PLD activation, mercury-induced PLD activation in MAECs, and agonist- and oxidant-induced PLD activation in a dose-dependent manner. |
| ln Vivo |
In vivo, FIPI rapidly blocks phosphatidic acid (PA) production with low nanomolar potency. It attenuates mercury-induced lipid signaling, resulting in protection against cytotoxicity in aortic endothelial cells. Detailed in vivo efficacy data in disease models are not provided.
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| Enzyme Assay |
Phospholipase D activity is quantified by measuring the formation of [³²P]-radiolabeled phosphatidylbutanol (PBt). Cellular lipids are extracted, and PBt is isolated using lipid extraction and thin-layer chromatographic separation. Radioactivity is measured using liquid scintillation counting and quantified as DPM normalized to total cellular lipid extract or as percentage of control.
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| Cell Assay |
Cytotoxicity is determined by assaying the extent of reduction of MTT in intact cells using a commercial MTT reduction assay kit. Cells are treated with FIPI HCl, followed by addition of MTT solution and incubation. Absorbance of reduced MTT is measured spectrophotometrically to assess cell viability.
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| Animal Protocol |
In vivo protocols for FIPI HCl are not detailed in the available references. As a research compound, it would typically be administered to animal models via intravenous or intraperitoneal injection to study its effects on PLD-mediated lipid signaling and associated biological processes.
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| ADME/Pharmacokinetics |
FIPI HCl has favorable pharmacokinetics with a half-life of greater than 5 hours, a Cmax of greater than 10-fold the IC50 versus PLD2, and moderate bioavailability of 18%. The molecular formula is C₂₃H₂₅ClFN₅O₂ with a molecular weight of 457.93. It typically exists as a solid at room temperature.
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| Toxicity/Toxicokinetics |
No specific toxicity data are detailed in the available references. As a PLD inhibitor, potential toxicities would depend on the importance of PLD-mediated signaling in various tissues. The compound's moderate bioavailability and favorable pharmacokinetics suggest it is being evaluated as a research tool.
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| References | |
| Additional Infomation |
FIPI HCl is a research compound not approved for clinical use. It is a potent and selective pharmacological tool for studying phospholipase D function in various biological processes including cell signaling, membrane trafficking, and inflammation. Its ability to block PA production makes it useful for investigating the role of PLD in disease models.
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| Molecular Formula |
C23H25CLFN5O2
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| Molecular Weight |
457.93
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| Exact Mass |
457.168
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| CAS # |
1781834-93-2
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| Related CAS # |
1781834-93-2 (HCl);939055-18-2;
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| PubChem CID |
90488864
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.FC1C=CC2=C(C=1)C=C(C(NCCN1CCC(CC1)N1C(NC3C=CC=CC1=3)=O)=O)N2
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| InChi Key |
BNMQCDOCYPGJJD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24FN5O2.ClH/c24-16-5-6-18-15(13-16)14-20(26-18)22(30)25-9-12-28-10-7-17(8-11-28)29-21-4-2-1-3-19(21)27-23(29)31;/h1-6,13-14,17,26H,7-12H2,(H,25,30)(H,27,31);1H
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| Chemical Name |
5-fluoro-N-[2-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]ethyl]-1H-indole-2-carboxamide;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1837 mL | 10.9187 mL | 21.8374 mL | |
| 5 mM | 0.4367 mL | 2.1837 mL | 4.3675 mL | |
| 10 mM | 0.2184 mL | 1.0919 mL | 2.1837 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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