A non-steroidal androgen receptor antagonist that is rapidly converted to 2-hydroxy flutamide in the liver by CYP1A2 and CYP3A4

Flutamide – 5 g

Brand:
Cayman
CAS:
13311-84-7
Storage:
22
UN-No:
Non-Hazardous - /

Flutamide is a non-steroidal androgen receptor antagonist that is rapidly converted to 2-hydroxy flutamide in the liver by cytochrome P450 (CYP) isoforms CYP1A2 and CYP3A4.{24727} Through competitive inhibition of the binding of testosterone to the nuclear androgen receptor (AR; IC50 = ~300-900 nM), 2-hydroxy flutamide blocks the expression of AR target genes and prevents androgen-dependent stabilization of the AR.{24726} Compared to its major metabolite, flutamide is a less potent antiandrogen in vivo. Thus, 2-hydroxy flutamide is the predominant contributor to the therapeutic effects of flutamide in the clinical treatment of prostate cancer.{22432}  

 

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Description

A non-steroidal androgen receptor antagonist that is rapidly converted to 2-hydroxy flutamide in the liver by CYP1A2 and CYP3A4

Formal name: 2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide

Synonyms:  Niftolide|NSC 147834|NSC 251876|SCH 13521

Molecular weight: 276.2

CAS: 13311-84-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Androgens

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