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Phloretin (Synonyms: NSC 407292, RJC 02792)

Catalog No.GC17976 Copy One-Click Copy Product Info

Phloretin is a dihydrochalcone flavonoid that inhibits yeast-derived GLUT1 and erythrocyte GLUT1 with IC50 values of 49μM and 61μM, respectively.

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Phloretin Chemical Structure

Cas No.: 60-82-2

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$31.00
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250mg
US$28.00
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500mg
US$36.00
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1g
US$47.00
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5g
US$84.00
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10g
US$109.00
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25g
US$164.00
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50g
US$205.00
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고객 리뷰

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of Phloretin

Phloretin is a dihydrochalcone flavonoid that inhibits yeast-derived GLUT1 and erythrocyte GLUT1 with IC50 values of 49μM and 61μM, respectively[1]. Phloretin displays potent antioxidant activity in peroxynitrite scavenging and the inhibition of lipid peroxidation, modulates Ca2+ levels and down-regulates the secretion of IL-2 of normal human lymphocytes, and counteracts advanced glycation end product formation[2]. Phloretin can penetrate the skin and has been widely used in dermatological research to prevent excessive skin pigmentation and skin damage[3].

In vitro, Phloretin treatment for 48 hours significantly inhibited the viability of HCT-116, SW-480, and IEC-6 cells, with IC50 values of 152.43µM, 127.50µM, and 412.56µM, respectively[4]. Treatment with 200µM Phloretin for 48 hours induced morphological changes in U87 and U251 cells, caused cell cycle arrest and accumulation of reactive oxygen species (ROS), inhibited the PI3K/Akt/mTOR signaling pathway, and increased the expression of PTEN[5]. Treatment with 75µg/ml Phloretin for 24 hours elicited apoptosis in A549 and Calu-1 cells, enhanced the expression of cleaved-caspase-3 and caspase-9, and decreased the levels of MMP-2 and MMP-9[6].

In vivo, Phloretin treatment via intraperitoneal injection at a dose of 20mg/kg, twice a week for 12 weeks, reduced the body weight and fat weight of obese mice on a high-fat diet (HFD), and alleviated hepatocyte steatosis[7]. Daily intraperitoneal injection of Phloretin (20mg/kg/day) for 7 days alleviated acute lung injury induced by lipopolysaccharide (LPS) in mice, inhibited neutrophil infiltration into lung tissue, and reduced the levels of IL-6 and TNF-α in serum and bronchoalveolar lavage fluid[8].

References:

[1] KASAHARA T, KASAHARA M. Expression of the rat GLUT1 glucose transporter in the yeast Saccharomyces cerevisiae[J]. Biochemical Journal, 1996, 315(1): 177-182.

[2] Behzad S, Sureda A, Barreca D, et al. Health effects of phloretin: from chemistry to medicine[J]. Phytochemistry reviews, 2017, 16(3): 527-533.

[3] Casarini T P A, Frank L A, Pohlmann A R, et al. Dermatological applications of the flavonoid phloretin[J]. European Journal of Pharmacology, 2020, 889: 173593.

[4] Kapoor S, Padwad Y S. Phloretin induces G2/M arrest and apoptosis by suppressing the β-catenin signaling pathway in colorectal carcinoma cells[J]. Apoptosis, 2023, 28(5): 810-829.

[5] Liu Y, Fan C, Pu L, et al. Phloretin induces cell cycle arrest and apoptosis of human glioblastoma cells through the generation of reactive oxygen species[J]. Journal of Neuro-oncology, 2016, 128(2): 217-223.

[6] Ma L, Wang R, Nan Y, et al. Phloretin exhibits an anticancer effect and enhances the anticancer ability of cisplatin on non-small cell lung cancer cell lines by regulating expression of apoptotic pathways and matrix metalloproteinases[J]. International Journal of Oncology, 2015, 48(2): 843-853.

[7] Liou C J, Wu S J, Shen S C, et al. Phloretin ameliorates hepatic steatosis through regulation of lipogenesis and Sirt1/AMPK signaling in obese mice[J]. Cell & Bioscience, 2020, 10(1): 114.

[8] Huang W C, Lai C L, Liang Y T, et al. Phloretin attenuates LPS-induced acute lung injury in mice via modulation of the NF-κB and MAPK pathways[J]. International immunopharmacology, 2016, 40: 98-105.

Protocol of Phloretin

Cell experiment [1]:

Cell lines

SW-480 cells

Preparation Method

SW-480 cells were cultured in Leibovitz’s L-15 medium, supplemented with 10% fetal bovine serum (FBS) and 1% antibiotic–antimycotic, at 37°C in an incubator with 5% CO2. Cells were inoculated at 4000 cells/well into 96-well plates and treated with Phloretin at various concentrations (10, 25, 50 100, 200, and 300µM) for 48h, the cell proliferation was tested.

Reaction Conditions

10, 25, 50 100, 200, and 300µM; 48h

Applications

Phloretin treatment reduced cell proliferation of SW-480 cells in a dose-dependent manner.
Animal experiment [2]:

Animal models

C57BL/6 mice

Preparation Method

C57BL/6 mice (4 weeks old) were randomly divided into 3 groups of 10. HFD based on research diets containing 23.1% protein, 34.9% fat, and 25.8% carbohydrates, and fat supplying 60% of energy. The normal control group (N) and HFD control group (HFD) were fed a standard chow diet or HFD, respectively, and administered DMSO solution by intraperitoneal injection. Phloretin groups were fed a HFD and administered 20mg/kg Phloretin by intraperitoneal injection (twice a week) for 12 weeks. Liver tissues from mice were collected for analysis.

Dosage form

20mg/kg; twice a week; 12 weeks; i.p.

Applications

Phloretin treatment suppressed liver lipid accumulation and improved hepatocyte steatosis in mice with HFD.

References:

[1] Kapoor S, Padwad Y S. Phloretin induces G2/M arrest and apoptosis by suppressing the β-catenin signaling pathway in colorectal carcinoma cells[J]. Apoptosis, 2023, 28(5): 810-829.

[2] Liou C J, Wu S J, Shen S C, et al. Phloretin ameliorates hepatic steatosis through regulation of lipogenesis and Sirt1/AMPK signaling in obese mice[J]. Cell & Bioscience, 2020, 10(1): 114.

Chemical Properties of Phloretin

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Phloretin

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.646 mL 18.2302 mL 36.4604 mL
5 mM 729.2 μL 3.646 mL 7.2921 mL
10 mM 364.6 μL 1.823 mL 3.646 mL
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Review for Phloretin

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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