依曲替酯 T6831

Product Introduction
Bioactivity


英文名: Etretinate

描述: Etretinate (Ro 10-9359) 是一种口服芳香族维甲酸，对牛皮癣和其他皮肤病综合征有效。 它激活类视黄醇受体，引起细胞分化的诱导、细胞增殖的抑制和炎症细胞对组织浸润的抑制。

细胞实验: The HSC-5 cells are plated in 96-well plates at a density of 1.5×103 per 100 μL and used for experiments. Preliminary experiments are performed to determine the effective dose and cytotoxicity of etretinate. The cells are incubated for 72 h with etretinate at concentrations of 5, 10, 25 and 50 nmol⁄L [dissolved in saline containing 0.0001% dimethyl sulfoxide (DMSO)]. The cells are then incubated for a further 2 h with or without 200 μmol⁄L ALA (Sigma). Each plate is then irradiated using a metal halide lamp at doses of 10, 20, 40 and 80 J⁄cm2 (Only for Reference)

体外活性: K03861 inhibits CDK2 activity by competing with binding of activating cyclins. [1]

体内活性: There is a significant decrease in mean dermal thickness (P < 0.05) and changes in collagen bundles in the etretinate-treated mice group for a 28-day period compared to control groups. TUNEL assay shows that the density of TUNEL-positive cells in the dermis of etretinate-treated mice for a 14-day period is significantly increased (P < 0.05). The ratio of procollagen α 1 (I) chain to β actin mRNA from etretinate-treated mice for a 1-day period decreased significantly compared to that of the control mice, but the ratio from etretinatetreated mice for a 14-day period increased significantly (P < 0.05)[2]. Etretinate reduces dermal thickness, and suppresses the appearance of skin lesions by inducting apoptosis and perhaps regulation of cytokine expression in MRL/lpr mice[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 65 mg/mL (183.4 mM)
Ethanol : 65 mg/mL (183.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | inhibit | Etretinate | Apoptosis

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相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Human Metabolite Library | Anti-Cancer Approved Drug Library | Apoptosis Compound Library | Orally Active Compound Library | NO PAINS Compound Library

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