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Pimethixene
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Catalog No. T12489Cas No. 314-03-4
Alias Pimetixene, Calmixen
Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).
Pimethixene
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Purity: 97.50%
Catalog No. T12489Alias Pimetixene, CalmixenCas No. 314-03-4
Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $29 | In Stock | In Stock | |
| 5 mg | $43 | In Stock | In Stock | |
| 10 mg | $59 | In Stock | In Stock | |
| 25 mg | $108 | In Stock | In Stock | |
| 50 mg | $160 | In Stock | In Stock | |
| 100 mg | $238 | In Stock | - | |
| 200 mg | $356 | Inquiry | Inquiry | |
| 1 mL x 10 mM (in DMSO) | $48 | 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:97.50%
Appearance:Solid
Color:White
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Product Introduction
Pimethixene AI Summary
Pimethixene is a molecule that exhibits a diverse range of bioactivities across various biological pathways. It has a high binding affinity for the 5-hydroxytryptamine 2A receptor from rat forebrain with a Ki value of 2.5 nM, suggesting potential effects on serotonin signaling pathways. In human H4 cells, it inhibits acid sphingomyelinase (ASM) with 32.0% residual activity at a concentration of 10 μM. Additionally, it inhibits LuxR-dependent quorum sensing in Vibrio fischeri with an IC50 of 56000.0 nM by reducing the bioluminescence intensity induced by 3-oxo-C6-HSL.
Pimethixene also demonstrates inhibition of recombinant SET7/9 with an IC50 of 4300.0 nM and the internalization of Anthrax Lethal Toxin with a potency of 10000.0 nM. It acts as both an inhibitor and a substrate for Cytochrome P450 enzymes 2C19 and 2D6 with potencies of 15848.9 nM and 3981.1 nM respectively. Furthermore, it shows inhibitory activity against USP1/UAF1 (IC50 35481.3 nM) and the Marburg Virus (IC50 8912.5 nM).
In the context of antiviral activity, Pimethixene exhibits low activity against SARS-CoV-2 in HRCE cells, and has a high IC50 value (> 100000.0 nM) for inhibiting VERO-6 cell cytotoxicity induced by the virus. It also shows cytotoxicity in VERO-E6 cells with a CC50 value of 25700.0 nM.
Notably, Pimethixene inhibits human HDAC6 enzyme activity with 47.37% inhibition observed in one enzyme assay, compared to 2.75% in another, indicating potential selectivity for HDAC6.
Finally, it interacts with various other receptors and enzymes, displaying bioactivity across a broad spectrum of targets including DRD1, SLC6A2, ADRA2A, HTR1A, DRD3, CHRM2, and TBXA2R, with agonistic activity towards TBXA2R and antagonistic activity towards CHRM1 and ADRA1A, though showing no significant activity against some targets like ESR1 and MAOA within tested concentration ranges..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively). |
| Targets&IC50 | 5-HT2A receptor:10.22 (pki), 5-HT2B receptor:10.44 (pki), D2 receptor:8.19 (pki), M1 mAChR:8.61 (pki), M2 mAChR:9.38 (pki), 5-HT2C receptor:8.42 (pki), 5-HT1A receptor:7.63 (pki), DD4.4 receptor:7.54 (pki), H1 receptor:10.14 (pki) |
| Synonyms | Pimetixene, Calmixen |
| Molecular Weight | 293.43 |
| Formula | C19H19NS |
| Cas No. | 314-03-4 |
| Smiles | CN1CCC(CC1)=C1c2ccccc2Sc2ccccc12 |
| Relative Density. | 1.192g/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: 18.33 mg/mL (62.47 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
Keywords
Serotonin ReceptorPimethixeneM2 receptorM2 mAChRM1 receptorM1 mAChRInhibitorinhibitHistamineReceptorHistamine ReceptorH1 receptorDopamineReceptorDopamine ReceptorDD4.4 receptorD4.4 receptorD2 receptorD25-hydroxytryptamine Receptor5HTReceptor5-HT2C Receptor5-HT2C5-HT2B Receptor5-HT2B5-HT2A Receptor5-HT2A5-HT1A Receptor5-HT1A5-HT Receptor5HT Receptor
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