Vorozole

Names

[ Name ]:
Vorozole

[Synonym ]:
Vorozolum
6-[(S)-(4-Chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole
(S)-6-[(4-Chlorophenyl)-1H-1,2,4-triazol-1-ylmethyl]-1-methyl-1H-benzotriazole
Vorozolum [INN-Latin]
(+)-(S)-6-(p-Chloro-α-1H-1,2,4-triazol-1-ylbenzyl)-1-methyl-1H-benzotriazole
Rivizor
1H-1,2,3-Benzotriazole, 6-[(S)-(4-chlorophenyl)-1H-1,2,4-triazol-1-ylmethyl]-1-methyl-
(+)-(S)-6-[4-Chloro-a-(1H-1,2,4-triazol-1-yl)benzyl]-1-methyl-1H-benzotriazole
Vorozole
Rivizor (TN)
Vorozol [INN-Spanish]
Vorozol
1H-Benzotriazole, 6-((4-chlorophenyl)-1H-1,2,4-triazol-1-ylmethyl)-1-methyl-, (S)-

Biological Activity

[Description]:

Vorozole is a potent and selective, orally active non-steroidal aromatase inhibitor[1][2]. Vorozole shows antitumor activity in vivo. Vorozole has the potential for the research of mammary cancer[3].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Aromatase

[In Vitro]

Vorozole inhibits aromatase activity with an IC50s of 1.4 nM in FSH-stimulated rat granulosa cells[4].

[In Vivo]

Vorozole (0.8-1.25 mg/kg; Gavage; daily for 77 dayss) shows antitumor effect and increase the release of serum insulin-like growth factor (IGF)-1 and serum testosterone levels[3]. Vorozole (p.o.; 5 days) dose-dependently reduced uterus weight and completely inhibited tumor aromatase in ovariectomized nude mice[4]. Animal Model: Female Sprague-Dawley rats[3] Dosage: 0.08, 0.16, 0.31, 0.63 or 1.25 mg/kg Administration: Gavage; daily (starting at 43 days of age) for 77 days; given a single i.v. dose of methylnitrosourea (MNU) (50 mg/kg body wt) after 7 days Result: Caused a dose-dependent increase in body weight gain and decrease in cancer incidence, increased the insulin-like growth factor (IGF)-1, serum testosterone levels.

[References]

[1]. Wouters W, et al. Pharmacology of vorozole. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):617-21.

[2]. Wiseman LR, et al. Vorozole. Drugs Aging. 1997 Sep;11(3):245-50; discussion 251-2.

[3]. Lubet RA,et al. Chemopreventive effects of the aromatase inhibitor vorozole (R 83842) in the methylnitrosourea-induced mammary cancer model. Carcinogenesis. 1998 Aug;19(8):1345-51.

[4]. Wouters W, et al. Pharmacology of vorozole. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):617-21.

Chemical & Physical Properties

[ Density]:
1.44g/cm3

[ Boiling Point ]:
575.1ºC at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₃ClN₆

[ Molecular Weight ]:
324.77

[ Flash Point ]:
301.6ºC

[ Exact Mass ]:
324.08900

[ PSA ]:
61.42000

[ LogP ]:
2.85090

[ Vapour Pressure ]:
3.15E-13mmHg at 25°C

[ Index of Refraction ]:
1.738

Safety Information

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%