Conditionnement : 100mg
Téléphone : +1 850 650 7790
Synonyms: MK-870 hydrochloride, Amiloride HCl
| Description | Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial. |
| Targets & IC50 | uPA:7 μM(Ki) |
| In vitro | In salt-sensitive hypertensive animals, Amiloride antagonizes or blocks the action of aldosterone in cells, as well as within vascular and renal tissues. Daily subcutaneous injections of 1 mg/kg Amiloride in DOCA-salt hypertensive rats reversed the initial increase in collagen deposition. In stroke-prone spontaneously hypertensive rats, Amiloride administration via saline drinking water delayed the onset of proteinuria and improved histological scores in brain and kidney tissues compared to controls. |
| In vivo | Upon increased perfusion pressure, 1 μM Amiloride and 30 nM Benzamil inhibit myogenic responses by blocking the activity of ENaC proteins, thereby suppressing vasoconstriction. In vascular smooth muscle cells, Amiloride completely inhibits sodium influx. Amiloride is a relatively selective inhibitor of epithelial sodium channels (ENaC) with an IC 50 of 0.1 μM to 0.5 μM. Although less effective as a Na+/H+ exchanger (NHE) inhibitor, Amiloride's IC 50 values range from as low as 3 μM at low external sodium concentrations to 1 mM at high external sodium concentrations. Furthermore, Amiloride exerts a weak inhibitory effect on Na+/Ca2+ exchange (NCX) with an IC 50 of 1 mM. |
| Synonyms | MK-870 hydrochloride, Amiloride HCl |
| Molecular Weight | 266.09 |
| Formula | C6H9Cl2N7O |
| Cas No. | 2016-88-8 |
| Smiles | Cl.NC(=N)NC(=O)c1nc(Cl)c(N)nc1N |
| Relative Density. | 2.11 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 | H2O: < 1 mg/mL (insoluble)  DMSO: 50 mg/mL (187.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.52 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 | ||||||||||||||||||||||||||||||||||||
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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