SR 11302 是激活蛋白-1 (AP-1) 转录因子抑制剂。SR 11302 是一种类视黄醇，可特异性抑制 AP-1 活性，而不会激活视黄酸反应元件 (RARE) 的转录。
| 生物活性 | SR 11302 is anactivator protein-1(AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibitsAP-1activity without activating the transcription of retinoic acid response element (RARE)[1]. |
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体外研究
(In Vitro) | SR 11302 (SR11302) show strong anti-AP-1 activity with selective binding with RARα and RARγ, but not with RARβ and RXRα[1].
SR 11302 (SR-11302; 1 μM) inhibits AP-1 transcription factor activity and decreases aldosterone levels by 61.9% in hypoxia-treated cells[2].
SR 11302 (SR-11302; 2 μM; 48 hours) inhibitsHelicobacter pylori(H. pylori)-induced cell proliferation in adenocarcinoma gastric (AGS) cells[3].
SR 11302 (2 μM; 24 hours) inhibitsH. pylori-induced expression of β-catenin and c-myc in AGS cells[3].
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体内研究
(In Vivo) | SR 11302 (SR11302; low dose 0.5 mg/kg and high dose 1 mg/kg body weight; orally gavaged daily) treatment reduces the total vascular lesion number and lesion size inVldlr-/-mice in a dose-dependent manner[4].
| Animal Model: | Vldlr-/-mice[4] | | Dosage: | Low dose 0.5 mg/kg and high dose 1 mg/kg body weight | | Administration: | Orally gavaged daily from P5 to P15 | | Result: | High-dose from P5 to P15 reduced the total vascular lesion number by 48% and decreased the lesion size by 40%, without detectable signs of toxicity in mice, including no change in body weight. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(66.40 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 2.6558 mL | 13.2792 mL | 26.5583 mL | | 5 mM | 0.5312 mL | 2.6558 mL | 5.3117 mL | | 10 mM | 0.2656 mL | 1.3279 mL | 2.6558 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。-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 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (6.64 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (6.64 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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