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Khellin
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Catalog No. T1431Cas No. 82-02-0
Alias Visammin, Methafrone, Amicardine
Khellin (Methafrone) is a vasodilator that also has bronchodilatory action.
Khellin
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Purity: 99.95%
Catalog No. T1431Alias Visammin, Methafrone, AmicardineCas No. 82-02-0
Khellin (Methafrone) is a vasodilator that also has bronchodilatory action.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $31 | In Stock | In Stock | |
| 25 mg | $47 | In Stock | In Stock | |
| 50 mg | $68 | In Stock | In Stock | |
| 100 mg | $89 | In Stock | In Stock | |
| 500 mg | $219 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $29 | 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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Purity:99.95%
Appearance:Solid
Color:White
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Product Introduction
Khellin AI Summary
Khellin is a versatile bioactive molecule exhibiting a range of pharmacological effects across various biological targets. It is effective in altering serum lipoprotein levels in normocholesterolemic male S.E.A. Japanese quail, increasing HDL cholesterol and decreasing VLDL+LDL cholesterol at a dosage of 50 mg/kg/day. The compound also shows vasorelaxation properties in rat aorta rings with IC50 values of 309,000 nM and 316,100 nM when pre-contracted with noradrenaline and KCl, respectively, and demonstrates antagonist activity with a PD'2 value of 4.46.
Additionally, Khellin has shown to inhibit HIV1 reverse transcriptase with an IC50 value greater than 200.0 µg/mL. It modulates various biological pathways and enzymes, including enhancing SMN2 splice variant expression, inhibiting Cytochrome P450 2C19 and 3A4 among others, and showing dual bioactivity against human tyrosyl-DNA phosphodiesterase 1 (TDP1) and Human Apurinic/apyrimidinic Endonuclease 1 (APE1). It also inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells and shows moderate inhibition of acetylcholinesterase and butyrylcholinesterase.
Moreover, Khellin has exhibited antibacterial and antifungal activities against several pathogens, including Klebsiella pneumoniae, Pseudomonas aeruginosa, and Candida albicans. It has shown antiviral properties against SARS-CoV-2 by inhibiting virus-induced cytotoxicity in VERO-6 cells and Caco-2 cells, with inhibition percentages varying depending on the assay and conditions.
Despite demonstrating potent inhibition of human CYP1A1 and CYP1A2 enzymes, Khellin is also associated with moderate liver toxicity, evidenced by elevated ALT or AST levels. Finally, its thermodynamic equilibrium solubility varies in solutions like water, PBS, and simulated gastric and intestinal fluids, which may impact its pharmacokinetic properties..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Khellin (Methafrone) is a vasodilator that also has bronchodilatory action. |
| Targets&IC50 | EGFR:0.15 µM (IC50) |
| Synonyms | Visammin, Methafrone, Amicardine |
| Molecular Weight | 260.24 |
| Formula | C14H12O5 |
| Cas No. | 82-02-0 |
| Smiles | COc1c2ccoc2c(OC)c2oc(C)cc(=O)c12 |
| Relative Density. | 1.301 g/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: 12 mg/mL (46.11 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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