Formaat : 1mLx10mM(inDMSO)
Telefoonnummer : +1 850 650 7790
Synonyms: SC-66110, Epoxymexrenone, CGP 30083
| Description | Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease. |
| Targets & IC50 | Aldosterone:0.36 μM |
| In vitro | Eplerenone increases total vascular and luminal areas in swine without affecting the endothelial area. In canine models, it significantly reduces left ventricular end-diastolic wall stress. Eplerenone attenuates the rise in pulse pressure due to aldosterone (Aldo) in rats, normalizing the wall stress curve, mean cross-sectional area, and EIIIA fibronectin levels in Aldo-salt hypertensive rats. The compound upregulates diminished endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats, markedly improving glomerulosclerosis and proteinuria. In mice, daily administration of 200 mg/kg of Eplerenone significantly lowers systolic and diastolic blood pressures compared to controls and increases serum phosphatase activity. |
| Synonyms | SC-66110, Epoxymexrenone, CGP 30083 |
| Molecular Weight | 414.49 |
| Formula | C24H30O6 |
| Cas No. | 107724-20-9 |
| Smiles | C[C@@]12[C@]34[C@]([C@]5([C@](C)(C[C@]3(O4)21)[C@@]6(CC5)CCC(=O)O6)21)([C@H](C(OC)=O)CC1=CC(=O)CC2)21 |
| Relative Density. | 1.31 g/cm3 (Predicted) |
| 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: 7.14 mg/mL (17.23 mM), Sonication is recommended.  | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: 0.71 mg/mL (1.71 mM), Solution. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.41 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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