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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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SR-11302 (SR11302) is an AP-1 (activator protein-1) transcription factor inhibitor with antitumor activity. SR11302 does not activate transcription from the retinoic acid response element (RARE) and displays no activity at retinoic acid receptors (EC50 > 1 μM for RARα, RARβ, RARγ and RXRα).
ln Vitro |
Strong anti-AP-1 activity is exhibited by SR 11302 (SR11302), which selectively binds to RARα and RARγ but not to RARβ or RXRα [1]. In cells treated with hypoxia, SR 11302 (SR-11302; 1 μM) decreases aldosterone levels by 61.9% and inhibits the activity of the AP-1 transcription factor [2]. Helicobacter pylori (H. pylori)-induced gastric adenocarcinoma (AGS) cell proliferation is inhibited by SR 11302 (SR-11302; 2 μM; 48 hours) [3]. In AGS cells, β-catenin and c-myc expression generated by Helicobacter pylori is inhibited by SR 11302 (2 μM; 24 hours) [3].
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ln Vivo |
Treatment with SR 11302 (SR11302; low dosage 0.5 mg/kg and high dose 1 mg/kg body weight; daily oral gavage) lowers total vascular lesion number and lesion size in Vldlr-/- mice in a dose-dependent manner [4] .
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Animal Protocol |
Animal/Disease Models: Vldlr-/- mice [4]
Doses: low dose 0.5 mg/kg and high dose 1 mg/kg Body weight Route of Administration: P5 to P15 Daily po (oral gavage) Experimental Results: P5 to P15 High dose reduces total vascular lesions The number was diminished by 48%, the lesion size was diminished by 40%, and no signs of toxicity were detected in the mice, including no changes in body weight. |
References |
[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. |
Molecular Formula |
C26H32O2
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Molecular Weight |
376.53108
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CAS # |
160162-42-5
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SMILES |
CC1=CC=C(C=C1)/C(=C\C=C\C(=C\C(=O)O)\C)/C=C/C2=C(C)CCCC2(C)C
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~25 mg/mL (~66.40 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.64 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2 mg/mL (5.31 mM) in 1% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.