SML2040
Liarozole dihydrochloride
≥98% (HPLC)
Synonym(s):
5-[(3-Chlorophenyl)(1H-imidazol-1-yl)methyl]-1H-benzimidazole, 6-[(3-Chlorophenyl)(1H-imidazol-1-yl)methyl]-1H-benzimidazole dihydrochloride, R 75251 dihydrochloride, R-75251 dihydrochloride, R75251 dihydrochloride
Sign In to View Organizational & Contract Pricing.
Select a Size
About This Item
Empirical Formula (Hill Notation):
C17H13ClN4 · 2HCl
CAS Number:
Molecular Weight:
381.69
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
room temp
Biochem/physiol Actions
Liarozole (R 75251, R75,251) is an orally active benzimidazole-based retinoic acid (RA) metabolism blocking agent (RAMBA) that targets multiple P450 enzymes, including aromatase (CYP19), 17-hydroxylase/17,20-lyase (CYP17A1), 11-hydroxylase (CYP11B1), and RA 4-hydroxylase (CYP26). Liarozole is more effective than ketoconazole in vivo (plasma RA enhancement = 2.5 ng/mL vs. 1.3 ng/mL 2 hr after respective oral dosage of 40 mg/kg in rats) and, in contrast to ketoconazole, Liarozole does not significantly affect circulating adrenal androgen levels. Liarozole is shown to effectively suppress androgen-dependent tumor expansion of R3327G Dunning prostate adenocarcinoma xenografts in rats (by 66% and 81% with 80 and 120 mg/kg/day p.o., respectively) independent of its androgen biosynthesis inhibition.
Orally active retinoic acid (RA) metabolism blocking agent (RAMBA) with higher in vivo efficay than ketoconazole.
Storage Class
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
This item has
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
R Van Ginckel et al.
The Prostate, 16(4), 313-323 (1990-01-01)
The antitumoral activity of a novel imidazole derivative, R 75,251, has been studied in the androgen-dependent R3327G Dunning prostate adenocarcinoma grafted subcutaneously in syngeneic rats. Dietary application resulting approximately in dose levels of 80, 120, and 160 mg/kg reduced tumor
Effects of cytochrome P-450 inhibitors on the in vivo metabolism of all-trans-retinoic acid in rats.
J P Van Wauwe et al.
The Journal of pharmacology and experimental therapeutics, 252(1), 365-369 (1990-01-01)
This study examines the effects of ketoconazole, R 75 251 and some other cytochrome P-450 inhibitors on the in vivo metabolism of all-trans-retinoic acid (RA) in normal rats. Oral treatment with ketoconazole or R 75 251 (40 mg/kg, -1 hr)
J Bruynseels et al.
The Prostate, 16(4), 345-357 (1990-01-01)
R 75251, a new imidazole derivative, inhibited the conversion of androgens to estrogens, of progestins to androstenedione and testosterone, and of 11-deoxycorticosterone to corticosterone in human placenta microsomes, subcellular fraction of rat testis, bovine adrenocortical mitochondria, in cultured rat granulosa
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service