102676-87-9

102676-87-9 structure
102676-87-9 structure
  • Name: (R)-Fadrozole
  • Chemical Name: (R)-Fadrozole
  • CAS Number: 102676-87-9
  • Molecular Formula: C14H13N3
  • Molecular Weight: 223.27
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2021-10-18 20:51:48
  • Modify Date: 2024-01-09 10:11:27
  • (R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor[1]. (R)-Fadrozole also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.[1][2].

Name (R)-Fadrozole
Description (R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor[1]. (R)-Fadrozole also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats.[1][2].
Related Catalog
Target

pIC50: 6.17 (human placental aromatase)

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.
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.

Molecular Formula C14H13N3
Molecular Weight 223.27
Hazard Codes Xi