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Apararenone

From Wikipedia, the free encyclopedia
Nonsteroidal antimineralocorticoid
Pharmaceutical compound
Apararenone
Clinical data
Other namesMT-3995
Routes of
administration
Oral
Drug classAntimineralocorticoid
Identifiers
  • N-[4-(4-fluorophenyl)-2,2-dimethyl-3-oxo-1,4-benzoxazin-7-yl]methanesulfonamide
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC17H17FN2O4S
Molar mass364.39 g·mol−1
3D model (JSmol)
  • CC1(C(=O)N(C2=C(O1)C=C(C=C2)NS(=O)(=O)C)C3=CC=C(C=C3)F)C
  • 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
  • Key:AZNHWXAFPBYFGH-UHFFFAOYSA-N

Apararenone (INN; development codeMT-3995) is anonsteroidalantimineralocorticoid which is under development byMitsubishi Tanabe Pharma for the treatment ofdiabetic nephropathies andnon-alcoholic steatohepatitis.[1][2][3] It was also previously being developed for the treatment ofhypertension, but development was discontinued for this indication.[1] Apararenone acts as a highlyselectiveantagonist of themineralocorticoid receptor (Ki < 50 nM), thereceptor foraldosterone.[1][2][3] As of 2017, it is inphase IIclinical trials.[1]

See also

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References

[edit]
  1. ^abcd"Apararenone - Mitsubishi Tanabe Pharma - AdisInsight".
  2. ^abYang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences".Curr Opin Pharmacol.27:78–85.doi:10.1016/j.coph.2016.02.005.PMID 26939027.
  3. ^abKolkhof P, Nowack C, Eitner F (2015)."Nonsteroidal antagonists of the mineralocorticoid receptor".Curr. Opin. Nephrol. Hypertens.24 (5):417–24.doi:10.1097/MNH.0000000000000147.PMID 26083526.S2CID 22113501.

External links

[edit]


Mineralocorticoids
Antimineralocorticoids
Synthesis modifiers
MRTooltip Mineralocorticoid receptor
Agonists
Antagonists


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