| Description | (R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC 50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.. |
| In vitro | The (-)-enantiomer with the S-absolute configuration was responsible for the high aromatase inhibitory activity of (R)-Fadrozole[1]. |
| In vivo | (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]. (R)-fadrozole (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: SHHF rats[2]Dosage: 0.24 and 1.2 mg/kg Administration: Daily; oral Result: Decreased plasma aldosterone levels and reversed preexistent left ventricular interstitial fibrosis. |
| Synonyms | FAD286, (R)-CGS 16949A free base, (R)-Fadrozole |
| molecular weight | 223.27 |
| Molecular formula | C14H13N3 |
| CAS | 102676-87-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 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. |