产品描述
(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..
体外活性
The (-)-enantiomer with the S-absolute configuration was responsible for the high aromatase inhibitory activity of (R)-Fadrozole[1].
体内活性
(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.
Cas No.
102676-87-9
分子式
C14H13N3
分子量
223.27
别名
(R)-Fadrozole;(R)-CGS 16949A free base;FAD286;(R)-Fadrozole
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years