2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. SGLT Endogenous Metabolite GLUT
  4. Phloretin

Phloretin  (Synonyms: NSC 407292; RJC 02792)

Cat. No.: HY-N0142 Purity: 99.67%
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Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.

For research use only. We do not sell to patients.

Phloretin Chemical Structure

Phloretin Chemical Structure

CAS No. : 60-82-2

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Based on 12 publication(s) in Google Scholar

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Phloretin Related Antibodies

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Description

Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively[1].Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation[4].

IC50 & Target[1]

SGLT1

 

SGLT2

 

Microbial Metabolite

 

GLUT1

 

GLUT2

 

In Vitro

Phloretin induced obvious cytotoxicity against BEL-7402 cells with IC50 of 89.23 μM[2].
? Phloretin (40-160 μM; 24 hours) induces BEL-7402 cell apoptosis though the mitochondrial pathway, the cells exposed to phloretin exhibits nuclear chromatin condensation and increased fluorescence intensity. The caspase-9 reaches the peak level at 12 h, and leak levels of caspase-6 and caspase-3 activities occurrs 18 and 24 h after the exposure, respectively[2].
? Phloretin (0-100 μM; 24 hours) has effects on transcription factors of adipogenesis in differentiated 3T3-L1 adipocytes, decreases PPAR-γ, C/EBPα and C/EBPβ as a dose-dependent manner[3].
? Phloretin (0-100 μM; 24 hours) has effects on the AMPK pathway in differentiated 3T3-L1 adipocytes, increases the phosphorylation of substrate ACC-1, AMPK in PT-treated cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Phloretin Related Antibodies

Apoptosis Analysis[2]

Cell Line: BEL-7402 cell
Concentration: 40-160 μM
Incubation Time: 24 hours
Result: Induced cell apoptosis and activated caspase 3, 6 and 9.

Western Blot Analysis[3]

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Inhibited PPAR-γ, C/EBPα and C/EBPβ expression.

Western Blot Analysis[3]

Cell Line: 3T3-L1 adipocytes
Concentration: 0 μM, 3 μM, 10 μM, 30 μM, 100 μM
Incubation Time: 24 hours
Result: Upregulated the expression of p-ACC-1, p-AMPK, p-AMPKα and β .
In Vivo

Phloretin (oral administration; 50 or 100?mg/kg; once daily) decreases oxidative stress and diminished levels of malondialdehyde (MDA) and hydrogen peroxide (Phloretin (口服给药；50 或 100 mg/kg；每天一次) 降低爪组织中的氧化应激和丙二醛 (MDA) 和过氧化氢 (H2O2) 的水平，降低血清中抗胶原抗体的生产率[3]。) in paw tissue, reduces productivity of anti-collagen antibodies in serum[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Collagen-Induced Arthritis (CIA) Mice[3]
Dosage: 50 or 100 mg/kg
Administration: Oral adminstration
Result: Showed mitigation of clinical symptoms of RA in addition to reduced inflammation of hind-limbs compared to the control group.
Molecular Weight

274.27

Formula

C15H14O5
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(C1=C(O)C=C(O)C=C1O)CCC2=CC=C(O)C=C2
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (182.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6460 mL 18.2302 mL 36.4604 mL
5 mM 0.7292 mL 3.6460 mL 7.2921 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6460 mL 18.2302 mL 36.4604 mL 91.1511 mL
5 mM 0.7292 mL 3.6460 mL 7.2921 mL 18.2302 mL
10 mM 0.3646 mL 1.8230 mL 3.6460 mL 9.1151 mL
15 mM 0.2431 mL 1.2153 mL 2.4307 mL 6.0767 mL
20 mM 0.1823 mL 0.9115 mL 1.8230 mL 4.5576 mL
25 mM 0.1458 mL 0.7292 mL 1.4584 mL 3.6460 mL
30 mM 0.1215 mL 0.6077 mL 1.2153 mL 3.0384 mL
40 mM 0.0912 mL 0.4558 mL 0.9115 mL 2.2788 mL
50 mM 0.0729 mL 0.3646 mL 0.7292 mL 1.8230 mL
60 mM 0.0608 mL 0.3038 mL 0.6077 mL 1.5192 mL
80 mM 0.0456 mL 0.2279 mL 0.4558 mL 1.1394 mL
100 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9115 mL
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Phloretin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phloretin60-82-2NSC 407292 RJC 02792NSC407292NSC-407292RJC02792RJC 02792RJC-02792SGLTEndogenous MetaboliteGLUTSodium-dependent glucose cotransportersGlucose transporterInhibitorinhibitorinhibit

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