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Apararenone

Chemical Structure : Apararenone

CAS No.: 945966-46-1

Apararenone (MT-3995;MT3995)

Catalog No.: PC-35937Not For Human Use, Lab Use Only.

Apararenone (MT-3995) is a highly selective and potent, nonsteroidal mineralocorticoid receptor (MR) antagonist with Ki of 104 nM, >360-fold selectivity over GR,AR,PR and ER receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Apararenone (MT-3995) is a highly selective and potent, nonsteroidal mineralocorticoid receptor (MR) antagonist with Ki of 104 nM, >360-fold selectivity over GR,AR,PR and ER receptors.
Apararenone (MT-3995) exhibited a more potent antihypertensive and organ-protective activity than steroidal MRA eplerenone in a primary aldosteronism rat model obtained by infusing aldosterone in uninephrectomized rats.

Physicochemical Properties

M.Wt 364.391
Formula C17H17FN2O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)methanesulfonamide

References

1. Kolkhof P, et al. Curr Opin Nephrol Hypertens. 2015 Sep;24(5):417-24.
2. Kolkhof P, et al. J Endocrinol. 2017 Jul;234(1):T125-T140.
3. Iijima T, et al. J Med Chem. 2022 Jun 2. doi: 10.1021/acs.jmedchem.2c00402.

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