Fadrozole (hydrochloride)

Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively). It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone (ACTH, Cay-24257) in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 µM, respectively). It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg. Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 µM). It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.Formal Name: 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, monohydrochloride. CAS Number: 102676-31-3. Synonyms: CGS 16949A. Molecular Formula: C14H13N3 . HCl. Formula Weight: 259.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 10 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 2 mg/ml. lambdamax: 229 nm. SMILES: N#CC(C=C1)=CC=C1C(CCC2)N3C2=CN=C3.Cl. InChi Code: InChI=1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14,/h4-7,9-10,14H,1-3H2,1H. InChi Key: UKCVAQGKEOJTSR-UHFFFAOYSA-N.