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F3806 Sigma

Fadrozole hydrochloride

≥98% (HPLC)

Synonym: 4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, Afema, CGS 16949A

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Properties

Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
InChI Key   UKCVAQGKEOJTSR-UHFFFAOYSA-N
assay   ≥98% (HPLC)
form   powder
solubility   DMSO: >20 mg/mL
originator   Novartis
storage temp.   room temp

Description

Packaging

10, 50 mg in glass bottle

Biochem/physiol Actions

Fadrozole is a nonsteroidal aromatase inhibitor. Fadrozole is a very potent and highly selective inhibitor of the aromatase enzyme system in vitro and estrogen biosynthesis in vivo. It inhibited the conversion of [4-14C]androstenedione to [4-14C]estrone by human placental microsomes in a competitive manner (Ki = 1.6 nM). At a substrate concentration 3-fold the Km, Fadrozole was 180 times more potent, as an inhibitor, than aminoglutethimide (Cat. No. A9657), exhibiting half-maximal inhibition at 1.7 nM as compared to 0.3 μM. In vivo, Fadrozole lowered ovarian estrogen synthesis by gonadotropin-primed, androstenedione treated, immature rats by 90% at a dose of 260 μg/kg (PO). In vivo, Fadrozole leads to sequelae of estrogen deprivation (e.g. regression of DMBA-induced mammary tumors) without causing adrenal hypertrophy in adult rats. It blocked aromatase by 50% in human breast cancer homogenates, live breast cancer cells, human placental microsomes, and porcine ovarian microsomes at concentrations of 0.008 to 0.02 μM.

Features and Benefits

This compound was developed by Novartis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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Safety & Documentation

Safety Information

Symbol 
Signal word 
Danger
Hazard statements 
Precautionary statements 
Personal Protective Equipment 
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
2
RTECS 
DI4952500

Documents

Certificate of Analysis

Protocols & Articles

Articles

Nuclear Receptors (Steroids)

Intracellular receptors (IRs) are a class of ligand-dependent transcription factors that include receptors for both steroid and non-steroid hormones. Upon binding their cognate hormone, these recepto...
Keywords: Anti-inflammatory agents, Apoptosis, Atomic absorption spectroscopy, Cancer, Cardiovascular, Cell proliferation, Diseases, Diuretics, Gene expression, Hormones, Infrared spectroscopy, Ligands, Metabolism, Metabolites, Transcription, Transduction

Peer-Reviewed Papers
15

References

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