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Esaxerenone (CS-3150)

Cat. No. M10479
Esaxerenone (CS-3150) Structure
Synonym:

CS-3150; XL-550

Size Price Availability
50mg USD 1440  USD1600 Out of stock
100mg USD 1980  USD2200 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist. It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 466.47
Formula C22H21F3N2O4S
CAS Number 1632006-28-0
Purity >99%
Solubility DMSO 93 mg/mL
Storage at -20°C
References

Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys
Makiko Yamada, et al. Xenobiotica. 2017 Dec;47(12):1090-1103. PMID: 27866463.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Esaxerenone (CS-3150), CS-3150; XL-550 supplier, inhibitors

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