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Clemastine
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Catalog No. T19966Cas No. 15686-51-8
Alias Mecloprodin, Meclastin, HS-592, HS592, HS 592
Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects.
Clemastine
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Purity: 99.21%
Catalog No. T19966Alias Mecloprodin, Meclastin, HS-592, HS592, HS 592Cas No. 15686-51-8
Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $32 | - | In Stock | |
| 10 mg | $51 | - | In Stock | |
| 25 mg | $89 | In Stock | In Stock | |
| 50 mg | $135 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $35 | - | 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:99.21%
Appearance:Oil
Color:Transparent
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Product Introduction
Clemastine AI Summary
Clemastine exhibits a comprehensive range of bioactivities and pharmacokinetic properties. It has a partition coefficient (logD6.5) of 1.65, delta logD value of -0.89, ionization constant (pKa) of 9.2, and an oral bioavailability of 49.0% in humans. Notably, it inhibits the uptake of 4-(4-(dimethylamino)styryl)-N-methylpyridinium at human OCT1 with an IC50 value of 4900.0 nM, showing 78.8% inhibition at a concentration of 100 uM.
Bioactivity assays reveal that Clemastine exhibits a moderate potency as an inhibitor of various Cytochrome P450 enzymes (2C19, 2D6, 3A4), as well as displays agonist and antagonist activities across numerous receptors and enzymes. It also inhibits 15-human lipoxygenase 2 and ATXN expression and interacts with a variety of receptors related to cancer cell targeting, genotoxicity, and virus entry inhibition.
Specifically, Clemastine shows affinity for histamine H1 central receptors, multiple dopamine receptors (D1-D3), serotonin receptors (5-HT1B, 5-HT2 family, 5-HT6), sigma receptors (Sigma1, Sigma2), as well as adrenergic and muscarinic acetylcholine receptors. Moreover, it has inhibitory activities on human CYP2C19 and CYP3A4, with a varying IC50 ratio depending on the substrate used.
In antiviral studies, Clemastine demonstrated activity against Ebolavirus and SARS-CoV-2, inhibiting viral entry and replication with IC50 values of 1100.0 nM and 2137.96 nM, respectively. It also shows significant interactions with enzymes such as HDAC6 and various PDEs, highlighting its broad spectrum of biochemical targets.
Despite its bioactivity, Clemastine shows potential hepatotoxicity, indicated by elevated levels of liver enzymes (ALT, AST, ALP) and associated symptoms such as liver damage and cirrhosis but no acute liver toxicity observed. Furthermore, it presents with a logD7.4 value favorable for bioavailability and distribution.
Overall, Clemastine's extensive interaction with multiple biological pathways and receptors presents it as a compound of significant pharmacological interest, although caution regarding liver toxicity is advised..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects. |
| Synonyms | Mecloprodin, Meclastin, HS-592, HS592, HS 592 |
| Molecular Weight | 343.89 |
| Formula | C21H26ClNO |
| Cas No. | 15686-51-8 |
| Smiles | [C@@](OCC[C@@H]1N(C)CCC1)(C)(C2=CC=C(Cl)C=C2)C3=CC=CC=C3 |
| Relative Density. | 1.31g/cm3 |
| Storage | keep away from moisture | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (72.7 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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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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