Talarozole,201410-53-9

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YZ剂描述：

产品名称：Talarozole

产品别名：n-[4-[2-乙基-1-(1H-1,2,4-噻唑-1-基)丁基]苯基]-2-苯并噻唑胺

英文别名：Rambazole;R115866;R-115866;R 115866

靶点：Cytochrome P450

CAS：201410-53-9

纯度：>98%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Talarozole(R115866) is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.

溶解性：DMSO : ≥ 36 mg/mL (95.36 mM)

体外研究：

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

体内研究：A maximum 84% inhibition of CYP26 activity at 0.5 hours post-dose is predicted based on Talarozole (TLZ) Cmax of 80 nM and a Ki 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 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.

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