MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Talarozole

CAS No. : 201410-53-9

MCE 站：Talarozole

产品活性：Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂 (RAMBA)，可提高内源性全反式维甲酸 (RA) 的细胞内水平。Talarozole 抑制 CYP26A1 和 CYP26B1，IC₅₀ 值分别为 5.4 和 0.46 nM。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：RAR/RXR  |  Cytochrome P450  |  Autophagy

In Vitro: When HepG2 cells are cotreated with atRA and Talarozole (1 μM), 4-OH-RA and 4-oxo-RA formation is significantly decreased.

In Vivo: A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) C_max of 80 nM and a K_i of 1 nM following a single dose of Talarozole. Due to the short Talarozole half-life (2.2 hrs) CYP26 activity is predicted to return to 100% by 12 hours. In agreement with the predictions, atRA concentrations are increased by 82, 63 and 60% at 4 hours post-dose in the serum, liver and testes, respectively, and concentrations returned to baseline by 24 hours. Following multiple doses of Talarozole, liver CYP26 mRNA and activity are increased suggesting autoinduction of CYP26 due to increased atRA concentrations. In agreement, atRA concentrations are elevated in serum and liver at all timepoints measured. This increase in atRA concentrations is associated with increased mRNA of the mitochondrial biogenesis markers PGC-1β and NRF-1 in comparison to control mice.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Metabolism/Protease Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Antioxidants Compound Library  |  Oxygen Sensing Compound Library  |  Retinoic acid  |  Verapamil hydrochloride  |  Apigenin  |  Fenofibrate  |  Bexarotene  |  Ketoconazole  |  1-Aminobenzotriazole  |  Itraconazole  |  Abiraterone  |  AM580  |  CD437  |  Clarithromycin  |  Atazanavir sulfate  |  Isavuconazole  |  Atovaquone  |  Memantine hydrochloride  |  Fenretinide  |  Galangin  |  Isotretinoin  |  AGN 193109  |  Magnolol  |  Naringin  |  AGN 194310  |  Metyrapone  |  Tamibarotene  |  Adapalene  |  Furafylline  |  Gemfibrozil  |  TTNPB

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。