A non-steroidal mineralocorticoid receptor antagonist
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Apararenone

Item No. 30671

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(4-fluorophenyl)-3,4-dihydro-2,2-dimethyl-3-oxo-2H-1,4-benzoxazin-7-yl]-methanesulfonamide
CAS Number
945966-46-1
Synonyms
  • MT-3995
Molecular Formula
C17H17FN2O4S
Formula Weight
364.4
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC1(C)OC2=CC(NS(C)(=O)=O)=CC=C2N(C3=CC=C(F)C=C3)C1=O
InChi Code
InChI=1S/C17H17FN2O4S/c1-17(2)16(21)20(13-7-4-11(18)5-8-13)14-9-6-12(10-15(14)24-17)19-25(3,22)23/h4-10,19H,1-3H3
InChi Key
AZNHWXAFPBYFGH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $64

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    10 mg

    $115

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    25 mg

    $192

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    50 mg

    $288

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    Product Description

    Apararenone is a non-steroidal mineralocorticoid receptor antagonist (Ki = 0.104 µM for the human receptor).1 It is selective for mineralocorticoid receptors over estrogen receptor α (ERα) and ERβ and glucocorticoid, progesterone, and androgen receptors (IC50s = >100 µM for all). Apararenone increases the urinary ratio of sodium to potassium in adrenalectomized rats in a dose-dependent manner. It inhibits aldosterone- and nephrectomy-induced increases in systolic blood pressure and urinary albumin levels, as well as myocardial necrosis and fibrosis, cardiac arterial degeneration, and renal tubule damage, in a rat model of renal hypertension when administered at doses of 3 or 10 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iijima, T., Katoh, M., Takedomi, K., et al. Discovery of apararenone (MT-3995) as a highly selective, potent, and novel nonsteroidal mineralocorticoid receptor antagonist. J. Med. Chem. 65(12), 8127-8143 (2022).