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Eplerenone

Cat. No. M3256
Eplerenone Structure
Synonym:

Epoxymexrenone

Size Price Availability Quantity
5mg USD 45  USD45 In stock
10mg USD 70  USD70 In stock
25mg USD 140  USD140 In stock
50mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Eplerenone (Epoxymexrenone) is a selective, competitive and oral aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen, and glucocorticoid receptors. Eplerenone may be used in studies of hypertension and heart failure following myocardial infarction.

Chemical Information
Molecular Weight 414.49
Formula C24H30O6
CAS Number 107724-20-9
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Andrew Lotery, et al. Eplerenone for chronic central serous chorioretinopathy in patients with active, previously untreated disease for more than 4 months (VICI): a randomised, double-blind, placebo-controlled trial

[2] Tina Sc Tam, et al. Eplerenone for hypertension

[3] Gerasimos Filippatos, et al. A randomized controlled study of finerenone vs. eplerenone in patients with worsening chronic heart failure and diabetes mellitus and/or chronic kidney disease

[4] Mitja Lainscak, et al. Safety profile of mineralocorticoid receptor antagonists: Spironolactone and eplerenone

[5] Allan Struthers, et al. A comparison of the aldosterone-blocking agents eplerenone and spironolactone

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