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Liarozole (dihydrochloride)
SKU
HY-106019C-10 mg
Category Reference compound
Tags Cancer; Metabolic Disease; Inflammation/Immunology, Cytochrome P450;RAR/RXR, Metabolic Enzyme/Protease;Vitamin D Related/Nuclear Receptor
$150 – $240
Products Details
Product Description
– Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties[1][2][3].
Web ID
– HY-106019C
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C17H15Cl3N4
References
– [1]Kuijpers AL, et al. The effects of oral liarozole on epidermal proliferation and differentiation in severe plaque psoriasis are comparable with those of acitretin. Br J Dermatol. 1998;139(3):380-389.|[2]Lucker GP, et al. Oral treatment of ichthyosis by the cytochrome P-450 inhibitor liarozole. Br J Dermatol. 1997;136(1):71-75.|[3]Wouters W, et al. Effects of liarozole, a new antitumoral compound, on retinoic acid-induced inhibition of cell growth and on retinoic acid metabolism in MCF-7 human breast cancer cells. Cancer Res. 1992;52(10):2841-2846.|[4]Pignatello MA, et al. Liarozole markedly increases all trans-retinoic acid toxicity in mouse limb bud cell cultures: a model to explain the potency of the aromatic retinoid (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl] benzoic acid. Toxicol Appl Pharmacol. 2002; 178(3):186-194.|[5]Van Wauwe J, et al. Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J Pharmacol Exp Ther. 1992;261(2):773-779.|[6]Stearns ME, et al. Liarozole and 13-cis-retinoic acid anti-prostatic tumor activity [published correction appears in Cancer Res 1993 Dec 1;53(23):5831]. Cancer Res. 1993;53(13):3073-3077.
CAS Number
– 1883548-96-6
Molecular Weight
– 381.69
Compound Purity
– 99.0
SMILES
– ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1.[H]Cl.[H]Cl
Clinical Information
– Phase 3
Research Area
– Cancer; Metabolic Disease; Inflammation/Immunology
Solubility
– DMSO : 50 mg/mL (ultrasonic)|H2O : ≥ 50 mg/mL
Target
– Cytochrome P450;RAR/RXR
Isoform
– CYP26
Pathway
– Metabolic Enzyme/Protease;Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
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