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Esaxerenone (CS-3150)

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

CS-3150; XL-550

Size Price Availability Quantity
5mg USD 280  USD280 In stock
10mg USD 420  USD420 In stock
50mg USD 1250  USD1250 In stock
100mg USD 1900  USD1900 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 466.47
Formula C22H21F3N2O4S
CAS Number 1632006-28-0
Form Solid
Solubility (25°C) DMSO 93 mg/mL
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] Makiko Yamada, et al. Xenobiotica. Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys

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


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