Isotretinoin (13-cis-Retinoic acid) 是一种具有口服活性的维生素 A 衍生物，常被用于重度痤疮的研究，具有抗癌活性。
| 生物活性 | Isotretinoin (13-cis-Retinoic acid) is an orally active vitamin A derivative and is often be used for the research of severe acne. Isotretinoin also shows anticancer activity[1][2]. |
| IC50& Target[2] | Human Endogenous Metabolite |
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体外研究
(In Vitro) | Isotretinoin (13-cis-Retinoic acid) may act as a pro-drug that is converted intracellularly to metabolites that are agonists for RAR and RXR nuclear receptors[1].
Isotretinoin is highly sensitive to air, heat, and light[3].
Isotretinoin (0-40 μM; 24-96 h) significantly inhibits HepG2 cell viability[4].
Isotretinoin (10 μM; 48 h) down-regulatesc-MYCmRNA expression and this is partially due to P1 or P2 promoter activity[4].
Cell Viability Assay[4] | Cell Line: | HepG2 | | Concentration: | 0.1, 0.5, 1, 5, 10, 20, and 40 μM | | Incubation Time: | 24, 48, 72, and 96 h | | Result: | Showed a significant reduction in cell viability (less than 30%) at 96 h for all doses. |
RT-PCR[4] | Cell Line: | HepG2 | | Concentration: | 10 μM | | Incubation Time: | 48 h | | Result: | Significantly reduced the expression ofc-MYCmRNA by ~80%. |
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体内研究
(In Vivo) | Isotretinoin (13-cis-Retinoic acid) (1.3-481 μg/L; inhalation exposure; 45 min daily for 2 weeks) is an effective lung cancer chemopreventive agent in A/J Mice[2].
Isotretinoin accelerates alveolar repair after exodontia in rats[3].
| Animal Model: | Male A/J mice, lung carcinogenesis model[2] | | Dosage: | 1.3, 20.7, or 481 μg/L | | Administration: | Inhalation exposure, 45 min daily for 2 weeks | | Result: | Reduced the tumor multiplicity. Caused up-regulation of lung tissue nuclear retinoic acid receptors (RARs) relative to vehicle-exposed mice, RARα (3.9-fold vehicle), RARβ (3.3-fold), and RARγ (3.7-fold) at 20.7 μg/L. |
| Animal Model: | Wistar rats, tooth extraction model[3] | | Dosage: | 7.5 mg/kg | | Administration: | Oral gavage, daily for 30 days | | Result: | Accelerated the process of alveolar repair, significantly decreased serum calcium levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, protect from light, stored under nitrogen *该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(166.42 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.3285 mL | 16.6423 mL | 33.2845 mL | | 5 mM | 0.6657 mL | 3.3285 mL | 6.6569 mL | | 10 mM | 0.3328 mL | 1.6642 mL | 3.3285 mL |
*请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.32 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.92 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.92 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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