Liarozole - CAS 115575-11-6
Catalog number: 115575-11-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C17H13ClN4
Molecular Weight:
308.771
COA:
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Targets:
Aromatase | Cytochrome P450
Description:
This active molecular has a potential antineoplastic activity. As a retinoic acid metabolism blocking agent (RAMBA), liarozole inhibits P450-dependent ATRA-4-hydroxylase to an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. Meanwhile, liarozole also inhibits aromatase that catalyzes estrogen biosynthesis in rating-limited step. In Aug 2005, clinical development was ongoing for Ichthyosis in Europe.In Jan 2006, Phase-II/III clinical trials in Ichthyosis was ongoing in Europe and in Canada.
Purity:
98%
Appearance:
Powder
Synonyms:
6-[(3-chlorophenyl)-imidazol-1-ylmethyl]-1H-benzimidazole, R 75251; R-75251; R75251
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
treatment for Ichthyosis
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
UGFHIPBXIWJXNA-UHFFFAOYSA-N
InChI:
InChI=1S/C17H13ClN4/c18-14-3-1-2-12(8-14)17(22-7-6-19-11-22)13-4-5-15-16(9-13)21-10-20-15/h1-11,17H,(H,20,21)
Canonical SMILES:
C1=CC(=CC(=C1)Cl)C(C2=CC3=C(C=C2)N=CN3)N4C=CN=C4
Current Developer:
Originator:Janssen Pharmaceutica
1.Oral liarozole in the treatment of patients with moderate/severe lamellar ichthyosis: results of a randomized, double-blind, multinational, placebo-controlled phase II/III trial.
Vahlquist A1, Blockhuys S, Steijlen P, van Rossem K, Didona B, Blanco D, Traupe H. Br J Dermatol. 2014 Jan;170(1):173-81. doi: 10.1111/bjd.12626.
BACKGROUND: Oral liarozole, a retinoic acid metabolism-blocking agent, may be an alternative to systemic retinoid therapy in patients with lamellar ichthyosis.
2.Liarozole inhibits transforming growth factor-β3--mediated extracellular matrix formation in human three-dimensional leiomyoma cultures.
Levy G1, Malik M2, Britten J2, Gilden M2, Segars J1, Catherino WH3. Fertil Steril. 2014 Jul;102(1):272-281.e2. doi: 10.1016/j.fertnstert.2014.03.042. Epub 2014 May 10.
OBJECTIVE: To investigate the impact of liarozole on transforming growth factor-β3 (TGF-β3) expression, TGF-β3 controlled profibrotic cytokines, and extracellular matrix formation in a three-dimensional (3D) leiomyoma model system.
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