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Talarozole

CAS No. : 201410-53-9

MCE 國際站：Talarozole

產(chǎn)品活性：Talarozole (R115866) 是一種口服性全反式維甲酸代謝阻斷劑 (RAMBA)，可提高內(nèi)源性全反式維甲酸 (RA) 的細胞內(nèi)水平。Talarozole 抑制 CYP26A1 和 CYP26B1，IC₅₀ 值分別為 5.4 和 0.46 nM。

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Vitamin D Related/Nuclear Receptor  |  Autophagy

作用靶點：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.

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