Bioactivity | Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor[1]. Dexfadrostat also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.[1][2]. |
Target | pIC50: 6.17 (human placental aromatase) |
Invitro | The (-)-enantiomer with the S-absolute configuration was responsible for the high aromatase inhibitory activity of Dexfadrostat[1]. |
In Vivo | Dexfadrostat ((R)-fadrozole; 0.24 and 1.2 mg/kg; daily; oral) and (S)-fadrozole similarly decreases plasma aldosterone levels, whereas urinary aldosterone excretion rate was reduced only by S-fadrozole[2].Dexfadrostat (0.24 and 1.2 mg/kg; daily; oral) effectively reverses preexistent left ventricular interstitial fibrosis by 50% (vs. 42% for canrenoate), S-fadrozole was devoid of an antifibrotic effect[2]. Animal Model: |
Name | Dexfadrostat |
CAS | 102676-87-9 |
Formula | C14H13N3 |
Molar Mass | 223.27 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Furet P, et al. Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds. J Med Chem. 1993;36(10):1393-1400. [2]. Minnaard-Huiban M, et al. Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone. Endocrinology. 2008;149(1):28-31. |