Size : 1mLx10mM(inDMSO)
Phone : +1 850 650 7790
Synonyms: HM30181A mesylate, HM30181 mesylate
| Description | Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor. |
| In vitro | Administration of Encequidar at concentrations of 0.1 or 1 nM resulted in a reduction of cell survival by 20% and 42% upon exposure to 100 nM and 1000 nM of NSC 125973, respectively [2]. |
| In vivo | When administered simultaneously, Encequidar demonstrates increased plasma concentrations with the microcapsule formulation compared to the powder, showing notable differences from 1 to 2 hours. The microcapsule formulation achieves a 1.7-fold quicker Tmax and a 1.6-fold greater AUC value than the powder (2.5±0.6 vs. 4.3±0.9 hours; 107.7±20.1 vs. 64.3±18.0 h ng/mL), indicating faster and more efficient absorption. This enhanced absorption of Encequidar in microcapsule format is likely attributed to its improved aqueous solubility and dissolution rates, facilitated by the conversion from crystalline to amorphous form and the reduction in particle size [1]. |
| Synonyms | HM30181A mesylate, HM30181 mesylate |
| Molecular Weight | 784.83 |
| Formula | C39H40N6O10S |
| Cas No. | 849675-87-2 |
| Smiles | CS(O)(=O)=O.COc1cc2CCN(CCc3ccc(cc3)-n3nnc(n3)-c3cc(OC)c(OC)cc3NC(=O)c3cc(=O)c4ccccc4o3)Cc2cc1OC |
| Relative Density. | no data available |
| 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: 62.5 mg/mL (79.64 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 6.25 mg/mL (7.96 mM), Suspension. 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 | |||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||
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.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.
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.
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