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Pirenperone
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Catalog No. T2599Cas No. 75444-65-4
Pirenperone is a putative 5-HT2 receptor antagonist with the central antiserotonergic and antidopaminergic action.
Pirenperone
Copy Product Info🥰Excellent
Purity: 99.2%
Catalog No. T2599Cas No. 75444-65-4
Pirenperone is a putative 5-HT2 receptor antagonist with the central antiserotonergic and antidopaminergic action.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $34 | In Stock | In Stock | |
| 5 mg | $72 | In Stock | In Stock | |
| 10 mg | $116 | In Stock | In Stock | |
| 25 mg | $239 | In Stock | In Stock | |
| 50 mg | $378 | In Stock | In Stock | |
| 100 mg | $558 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.2%
Appearance:Solid
Color:White
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Product Introduction
Pirenperone AI Summary
Pirenperone exhibits bioactivity primarily related to serotonin receptors, demonstrating high binding affinity to the 5-HT2 receptor subtype in rat cortical membranes, with Ki values as low as 0.3 nM and moderate affinity for the 5-HT2C receptor subtype with a Ki value of 60 nM. It also shows lower binding affinity to 5-HT1A and 5-HT1B receptor subtypes. Additionally, it acts as a potent inhibitor of membrane-bound and solubilized receptors in rat frontal cortex, with IC50 values of 1.82 nM and 7.079 nM, respectively, pointing to high receptor affinity.
However, Pirenperone exhibits notable cardiotoxicity in Dunkin-Hartley guinea pigs, significantly prolonging the QTc interval. Moreover, the compound displays broad-spectrum bioactivity, including antiplasmodial effects against Plasmodium falciparum with IC50 values ranging from 6309.57 nM to 12589.25 nM and activity against other pathogens including Leishmania, Chagas disease, and HAT with varying IC50 values.
It also shows antiviral capabilities, inhibiting SARS-CoV-2 induced cytotoxicity in VERO-6 cells and specifically targeting the SARS-CoV-2 3CL-Pro protease enzyme. Moreover, it possesses antifungal and antibacterial activities, albeit with modest inhibition percentages.
Despite its diverse bioactivities, Pirenperone has weak inhibitory effects on the human HDAC6 enzyme, with minimal inhibition percentages observed. These extensive biological interactions suggest that Pirenperone may have potential therapeutic applications but also significant safety considerations..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Pirenperone is a putative 5-HT2 receptor antagonist with the central antiserotonergic and antidopaminergic action. |
| Molecular Weight | 393.45 |
| Formula | C23H24FN3O2 |
| Cas No. | 75444-65-4 |
| Smiles | O=C1N2C(=NC(C)=C1CCN3CCC(C(=O)C4=CC=C(F)C=C4)CC3)C=CC=C2 |
| Relative Density. | 1.26g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||
| Solubility Information | DMSO: 3.67 mg/mL (9.33 mM), Sonication is recommended.  | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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