Apararenone
Apararenone Basic information
- Product Name:
- Apararenone
- Synonyms:
-
- Apararenone
- MT-3995
- Methanesulfonamide, N-[4-(4-fluorophenyl)-3,4-dihydro-2,2-dimethyl-3-oxo-2H-1,4-benzoxazin-7-yl]-
- N-(4-(4-Fluorophenyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl)methanesulfonamide
- inhibit,Inhibitor,Mineralocorticoid Receptor,MT 3995,Apararenone,MT3995
- Apararenone/MT-3995
- Apararenone, 10 mM in DMSO
- CAS:
- 945966-46-1
- MF:
- C17H17FN2O4S
- MW:
- 364.39
- Mol File:
- 945966-46-1.mol
Apararenone Chemical Properties
- Boiling point:
- 594.3±60.0 °C(Predicted)
- Density
- 1.389±0.06 g/cm3(Predicted)
- solubility
- DMSO: Sparingly soluble: 1-10 mg/ml
- form
- Solid
- pka
- 8.02±0.40(Predicted)
- color
- White to off-white
Apararenone Usage And Synthesis
Uses
Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
in vivo
Recently, a phase II clinical trial has been initiated among patients with non-alcoholic steatohepatitis (NASH) in Japan[1].
References
[1] Kolkhof P, et al. 30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development. J Endocrinol. 2017 Jul;234(1):T125-T140. DOI:10.1530/JOE-16-0600
[2] TORU IIJIMA*, TAKAYUKI KAWAGUCHI Discovery of Apararenone (MT-3995) as a Highly Selective, Potent, and Novel Nonsteroidal Mineralocorticoid Receptor Antagonist[J]. Journal of Medicinal Chemistry, 2022, 65 12: 8127-8143. DOI: 10.1021/acs.jmedchem.2c00402
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