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Promethazine
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Catalog No. T0445Cas No. 60-87-7
Alias Proazamine, Diphergan
Promethazine (Proazamine) is an analogue of anti-glaucoma prostaglandin (PG) .
Promethazine
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Purity: 99.76%
Catalog No. T0445Alias Proazamine, DipherganCas No. 60-87-7
Promethazine (Proazamine) is an analogue of anti-glaucoma prostaglandin (PG) .
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $37 | In Stock | In Stock | |
| 10 mg | $50 | In Stock | In Stock | |
| 25 mg | $68 | In Stock | In Stock | |
| 50 mg | $109 | In Stock | In Stock | |
| 100 mg | $143 | In Stock | In Stock | |
| 500 mg | $336 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $40 | 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:99.76%
Appearance:Solid
Color:White
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Product Introduction
Promethazine AI Summary
Promethazine is a multi-faceted compound exhibiting a diverse range of biological activities. It inhibits the binding of Batrachotoxinin [3H]BTX-B to voltage-dependent sodium channels in guinea pig cerebral cortex with an IC50 of 6900.0 nM, achieving 61% inhibition at a concentration of 10 µM. It also demonstrates antimicrobial activity against Plasmodium falciparum with an IC50 of 20000.0 nM and against Trypanosoma cruzi Trypanothione reductase with an IC50 of 271000.0 nM and a Ki of 216000.0 nM. Additionally, it inhibits half-maximal Prion protein PrPsc formation in ScN2a cells with an EC50 of 8000.0 nM.
Physicochemically, Promethazine has a pKa ranging around 8.9 to 9.1, a logP of 4.81, and a logD7.4 of 2.67, indicating high plasma protein binding (92.95%). The compound shows a volume of distribution (Vdss) of 14.0 L.kg-1, total body clearance of 14.0 mL.min-1.kg-1, and renal clearance of 0.14 mL.min-1.kg-1. It has significant protein binding characteristics with a low fraction unbound (Fu) of 0.07.
In cellular assays, Promethazine shows various inhibitory activities including Na+/K+ ATPase in rat brain and histamine release from rat mast cells. It inhibits acid sphingomyelinase (ASM) in rat PC12 cells, demonstrating residual activity of 32.2% at 10 µM. It also shows higher LDH enzyme levels impacting liver and muscle health markers. Its histone lysine methyltransferase inhibition indicates potential epigenetic modulation.
Also, Promethazine has shown consistency in antiviral assays by inhibiting SARS-CoV-2 in VERO-6 cells with varying IC50 values and inducing limited liver toxicity. It demonstrates inhibitory activities on human CaV2.2 and quorum sensing systems in various bacteria strains. Its impact on clathrin-mediated endocytosis is notable with an IC50 of 7480.0 nM.
Overall, Promethazine's extensive bioactivity profile, including receptor binding, enzyme inhibition, antimicrobial actions, and physicochemical properties, suggests potential therapeutic applications across multiple disease models, necessitating further investigation into its biological interactions and therapeutic efficacy..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Promethazine (Proazamine) is an analogue of anti-glaucoma prostaglandin (PG) . |
| Synonyms | Proazamine, Diphergan |
| Molecular Weight | 284.42 |
| Formula | C17H20N2S |
| Cas No. | 60-87-7 |
| Smiles | CC(CN1C2=C(SC3=C1C=CC=C3)C=CC=C2)N(C)C |
| Relative Density. | 1.131 |
| 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: 11.01 mg/mL (38.71 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.03 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
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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