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Submit ReviewLiarozole dihydrochloride is a cytochrome P450 inhibitor. Inhibits several cytochrome P450 enzymes including aromatase (CYP19) and retinoic acid 4-hydroxylase (CYP26). Blocks retinoic acid metabolism (retinoic acid metabolism blocking agent, RAMBA). Displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.
Liarozole dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 381.69 |
公式 | C17H13ClN4.2HCl |
储存 | Desiccate at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 1883548-96-6 |
PubChem ID | 121513844 |
InChI Key | NKDMRTVUEJWCCQ-UHFFFAOYSA-N |
Smiles | ClC1=CC(C(N4C=CN=C4)C2=CC=C(N=CN3)C3=C2)=CC=C1.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.17 | 100 | |
water | 34.52 | 100 |
以下数据基于产品分子量 381.69。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.62 mL | 13.1 mL | 26.2 mL |
5 mM | 0.52 mL | 2.62 mL | 5.24 mL |
10 mM | 0.26 mL | 1.31 mL | 2.62 mL |
50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
参考文献是支持产品生物活性的出版物。
Van Wauwe et al (1992) Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J.Pharmacol.Exp.Ther. 261 773 PMID: 1374473
Njar et al (2006) Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases. Bioorg.Med.Chem. 14 4323 PMID: 16530416
Goss et al (2007) Effects of liarozole fumarate (R85246) in combination with tamox. on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model. BMC Cancer 7 26 PMID: 17266767
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关键词: Liarozole dihydrochloride, Liarozole dihydrochloride supplier, Cytochrome, P450, CYP26, inhibitors, inhibits, blocks, retinoic, acid, metabolism, Blocks, RXR, Retinoid, X, Receptors, CYP, RAR, RAMBA, Retinoic, Acid, R75251, R-75251, Receptor, 2705, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Liarozole dihydrochloride 的部分引用包括:
Bunt et al (2016) Insights into islet development and biology through characterization of a human iPSC-derived endocrine pancreas model. Islets 8 83 PMID: 27246810
Bhattacharya et al (2016) Normalizing Microbiota-Induced Retinoic Acid Deficiency Stimulates Protective CD8+ T Cell- Mediated Immunity in Colorectal Cancer Immunity 45 1 PMID: 27590114
Thomas and Henry (2014) Retinoic acid regulation by CYP26 in vertebrate lens regeneration. Neuropsychopharmacology 386 291 PMID: 24384390
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