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Temarotene

产品编号 T17034 CAS 75078-91-0

别名: Ro 15-0778

Temarotene（Ro 15-0778）是一种具有口服活性和有效性的小分子化合物，可在体外调节人体免疫功能。Temarotene 可用于研究扁平苔藓。

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Temarotene, CAS 75078-91-0

规格	价格/CNY		货期	数量
1 mg	￥ 4,900		现货
5 mg	￥ 12,600		现货

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其他形式的 Temarotene:

ONO4057
现货

选择批次

纯度: 97.54%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Temarotene (Ro 15-0778) is an orally active and potent small molecule compound that modulates human immune function in vitro.Temarotene may be used in the study of lichen planus.
靶点活性	ODC mRNA:0.5 μM
体外活性	The modulation of ornithine decarboxylase (ODC) gene expression by retinoids is analyzed in human keratinocyte cultures maintained in serum-free medium containing 0.15 mM Ca2+. Cells are incubated with all-trans-retinoic acid, 13-cis-retinoic acid, or arotinoid Ro15-0778 (0.1 nM to 10 μM). Total RNA is isolated, and mRNA transcripts for ODC are analyzed by Northern and slot blot hybridizations with a human ODC cDNA. Treatment of cells for 24 h results in a dose-dependent decrease in ODC mRNA levels, with an estimated IC50 of approximately 10 nM for all-trans- and 13-cis-retinoic acid, while Ro15-0778 is somewhat less effective (IC50 approximately 0.1-0.5 μM). The suppression of ODC mRNA levels by retinoids is detectable at approximately 3 h of incubation, with essentially maximal inhibition at 12 h. Reduced ODC mRNA levels noted after 24 h of incubation with 0.5 μM all-trans-retinoic acid are accompanied by a reduction in ODC enzyme activity[2].
体内活性	The aim of this preliminary report is to measure plasma and skin concentrations of Ro 15-0778 and its phenolic metabolite Ro 14-6113 in hairless rats receiving orally 10 mg/kg of Temarotene once daily during 10 days. Blood samples (2-3 mL) and skin samples (200-300 mg) are taken at different time points between 0.5 and 240 h after the last dose. A highly sensitive HPLC method is used for the simultaneous determination of the two compounds with a quantification limit of 2 ng/mL in plasma and 10 ng/g in total skin (epidermis and dermis). After 10 h, plasma concentrations of Ro 14-6113 are 5-13 times higher than for Ro 15-0778. Ro 14-6113 concentrations in the skin are 4-10 times higher than for Ro 15-0778 within the initial 48 h. The concentrations of both compounds in the skin are higher than concentrations in plasma[2].

别名	Ro 15-0778
分子量	304.47
分子式	C23H28
CAS No.	75078-91-0

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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稀释计算器

配液计算器

分子量计算器

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参考文献

1. Fenina N, et al. Concentration of Temarotene (Ro 15-0778) and its metabolite Ro 14-6113 in plasma and skin of hairless rat. Skin Pharmacol. 1993;6(1):61-4. 2. Olsen DR, et al. Suppression of ornithine decarboxylase gene expression by retinoids in cultured human keratinocytes. J Invest Dermatol. 1990 Jan;94(1):33-6.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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