Phloretin
(Synonyms: 根皮素; NSC 407292; RJC 02792) 目录号 : GC17976
A natural inhibitor of various transporters
Cas No.:60-82-2
Sample solution is provided at 25 µL, 10mM.
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Phloretin is a dihydrochalcone, a type of natural phenols which can be found in apple tree leaves and Manchurian apricot. Phloretin inhibits the active transport of glucose into cells via sodium-glucose linked transporter (SGLT) 1 and 2 with IC50 value of 49±12 μM [2].
SGLTs are a family of glucose transporter which is found in the small intestine mucosa (SGLT 1) and nephron proximal tubule (SGLT 2). They contribute to the renal glucose reabsorption.
After treatment of phloretin, differentiated 3T3-L1 cells exhibited significantly enhanced glycerol and the inhibition of adipogenesis-related transcription factor that were regulated by SGLTs. Additionally, phloretin promoted phosphorylation of AMP-activated protein kinase and increased activity of adipose triglyceride lipase and hormone-sensitive lipase [1]. When RAW 263.7 cells were cultured from differentiated 3T3-L1 cell media, PT suppressed the SGLT-associated nuclear transcription factor kappaB and mitogen-activated protein kinase pathways [1].
In streptozotocin-induced rat model of diabetes type I, oral administration of phloridzin (5/10/20/40 mg/kg/day) resulted in significant reduction of blood glucose levels and improved dyslipidemia. Additionally, Administration of phloridzin reduced urine volume and water intake in a dose-dependent manner [3].
References:
[1] Huang W C et al. , Phloretin and phlorizin promote lipolysis and inhibit inflammation in mouse 3T3-L1 cells and in macrophage-adipocyte co-cultures. Mol Nutr Food Res. 2013, 57: 1807-1817.
[2] Kasahara T, Kasahara M. Expression of the rat GLUT1 glucose transporter in the yeast Saccharomyces cerevisiae. Biochem J. 1996, 315 ( Pt 1):177-182.
[3] Najafian M, Jahromi M Z, Nowroznejhad M J, Phloridzin reduces blood glucose levels and improves lipids metabolism in streptozotocin-induced diabetic rats. Mol Biol Rep. 2012, 39(5): 5299-306.
| Cell experiment [1]: | |
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Cell lines |
U87 and U251 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >9.25mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0-300 μM; 12, 24, and 48 h; 37°C |
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Applications |
In U87 and U251 cell lines, Phloretin inhibited colony formation in a concentration-dependent manner. Phloretin also inhibited cell growth in a concentration- and time-dependent way. In U87 cells, Phloretin induced cell cycle arrest at the G0-G1 phase and significantly induced apoptosis. Phloretin also triggered the mitochondrial apoptosis pathway and generated reactive oxygen species (ROS). |
| Animal experiment [2]: | |
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Animal models |
ovalbumin (OVA)-induced asthmatic mice |
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Dosage form |
5, 10, or 20 mg/kg; intraperitoneally injection |
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Application |
In ovalbumin (OVA)-induced asthmatic mice, Phloretin (PT) could significantly diminish airway hyperresponsiveness (AHR). Phloretin significantly reduced numbers of eosinophils and total cells in bronchoalveolar lavage fluid (BalF). Phloretin also decreased malondialdehyde levels in the lung and reduced Th2 cytokine production in bronchoalveolar lavage fluids. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Huang WC1, Fang LW2, Liou CJ3, et al. Phloretin Attenuates Allergic Airway Inflammation and Oxidative Stress in Asthmatic Mice. Front Immunol. 2017 Feb 13;8:134. [2] Najafian M, Jahromi M Z, Nowroznejhad M J, Phloridzin reduces blood glucose levels and improves lipids metabolism in streptozotocin-induced diabetic rats. Mol Biol Rep. 2012, 39(5): 5299-306. | |
| Cas No. | 60-82-2 | SDF | |
| 别名 | 根皮素; NSC 407292; RJC 02792 | ||
| 化学名 | 3-(4-hydroxyphenyl)-1-(2,4,6-trihydroxyphenyl)propan-1-one | ||
| Canonical SMILES | O=C(C1=C(O)C=C(O)C=C1O)CCC2=CC=C(O)C=C2 | ||
| 分子式 | C15H14O5 | 分子量 | 274.27 |
| 溶解度 | ≥ 105 mg/mL in DMSO, ≥ 87.6 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.646 mL | 18.2302 mL | 36.4604 mL |
| 5 mM | 0.7292 mL | 3.646 mL | 7.2921 mL |
| 10 mM | 0.3646 mL | 1.823 mL | 3.646 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet