产品信息
抗原名称
Cytochrome P450
商品描述
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.
分子量
377.51
纯度
>98%
可溶性
DMSO : ≥ 36 mg/mL (95.36 mM)
外观
Powder
In vitro(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.
In vivo(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 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.
背景
别名
Rambazole；R115866；R-115866；R 115866
分子式
C21H23N5S
CAS号
201410-53-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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