Phloretin (Synonyms: NSC 407292, RJC 02792) |
| Catalog No.GC17976 |
A natural inhibitor of various transporters
Products are for research use only. Not for human use. We do not sell to patients.
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]: | |
|
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. |
|
Reacting condition |
0-300 μM; 12, 24, and 48 h; 37°C |
|
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 |
|
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. |
|
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. |
|
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 | |
| Synonyms | NSC 407292, RJC 02792 | ||
| Chemical Name | 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 | ||
| Formula | C15H14O5 | M.Wt | 274.27 |
| Solubility | ≥ 105 mg/mL in DMSO, ≥ 87.6 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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