9-cis-Retinoic acid (ALRT1057)，维生素 A 的衍生物，是一种有效的RAR/RXR激动剂。9-cis-Retinoic acid 可诱导细胞凋亡 (apoptosis)，调节细胞周期并具有抗癌，抗炎和神经保护活性。
| 生物活性 | 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potentRAR/RXRagonist. 9-cis-Retinoic acid inducesapoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5]. |
| IC50& Target | Human Endogenous Metabolite |
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体外研究
(In Vitro) | 9-cis-Retinoic acid (1-10 μM; 0-5 days; CA 9-22 and NA cells) treatment significantly decreases proliferation in a dose-dependent manner in CA 9-22 and NA cells[1].
9-cis-Retinoic acid (1 μM; 24 hours) treatment significantly increases PPARγ functional activity by >200% in CA 9-22 and NA aerodigestive cells[1].
9-cis-Retinoic acid treatment results in the formation of a nuclear PPARγ-RXRα heterodimer supershift complex in CA 9-22 cells[1].
9-cis-Retinoic acid inhibits proliferation and induces apoptosis in cutaneous T-cell lymphoma (CTCL) in a dose-dependent and time-dependent manner. 9-cis-Retinoic acid also induces G0/G1 cell cycle arrest by downregulation of cyclin D1. 9-cis-Retinoic acid significantly decreases phosphorylation of JAK1, STAT3, and STAT5 and downregulated Bcl-xL and cyclin D1[2].
Cell Proliferation Assay[1] | Cell Line: | CA 9-22 and NA cells | | Concentration: | 1 μM, 10 μM | | Incubation Time: | 0 day, 1 day, 3 days, 5 days | | Result: | Significantly decreased proliferation. |
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体内研究
(In Vivo) | 9-cis-Retinoic acid (1 mg/kg; intravenous injection; daily; for 10 days; male C57BL/6J mice) treatment significantly decreases the serum ALT and AST level, alleviates hepatic necrosis of the bile duct ligation (BDL)-mice[3].
| Animal Model: | Male C57BL/6J mice (6-8 weeks; 19-22 g) treatment with bile duct ligated[3] | | Dosage: | 1 mg/kg | | Administration: | Intravenous injection; daily; for 10 days | | Result: | Significantly decreased the serum ALT and AST level, alleviated hepatic necrosis. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(83.21 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 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); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.32 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (8.32 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.32 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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