SR 11302

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SR 11302  纯度: ≥98.0%

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。

SR 11302

SR 11302 Chemical Structure

CAS No. : 160162-42-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4400 In-stock
5 mg ¥4000 In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

生物活性

SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE)[1].

IC50 & Target

AP-1[1]

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) inhibits Helicobacter pylori (H. pylori)-induced cell proliferation in adenocarcinoma gastric (AGS) cells[3].
SR 11302 (2 µM; 24 hours) inhibits H. pylori-induced expression of β-catenin and c-myc in AGS cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 in Vldlr-/- mice in a dose-dependent manner[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

376.53

Formula

C26H32O2

CAS 号

160162-42-5

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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (265.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. C Huang, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A. 1997 May 27;94(11):5826-30.

    [2]. Bradley A Maron, et al. Upregulation of steroidogenic acute regulatory protein by hypoxia stimulates aldosterone synthesis in pulmonary artery endothelial cells to promote pulmonary vascular fibrosis. Circulation. 2014 Jul 8;130(2):168-79.

    [3]. Eunyoung Byun, et al. Activation of NF-κB and AP-1 Mediates Hyperproliferation by Inducing β-Catenin and c-Myc in Helicobacter pylori-Infected Gastric Epithelial Cells. Yonsei Med J. 2016 May;57(3):647-51.

    [4]. Ye Sun, et al. Inflammatory signals from photoreceptor modulate pathological retinal angiogenesis via c-Fos. J Exp Med. 2017 Jun 5;214(6):1753-1767.

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