Phloretin (Synonyms: NSC 407292; RJC 02792)

Name: Phloretin
Brand: MedChemExpress
SKU: HY-N0142
Rating: 5.0 (16 reviews)

Cat. No.: HY-N0142 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 60-82-2

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10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
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Based on 16 publication(s) in Google Scholar

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Phloretin (Standard) Get quote

16 Publications Citing Use of MCE Phloretin

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SGLT1 SGLT2

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GLUT1 GLUT2 GLUT3 GLUT4

Biological Activity
Purity & Documentation
References
Customer Review

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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	12.4 μM Compound: 9h	Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay	[PMID: 28098449]
HEK293	IC₅₀	18.3 μM Compound: 9h	Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay	[PMID: 28098449]
HEK293	IC₅₀	90 μM Compound: 4788	Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2 Inhibition of the Sodium/Hydrogen Exchanger-Like Domain-Containing Protein 2 (NHA2, SLC9B2) as assessed by a sensor pH-sensitive genetically encoded fluorescent sensor (pHAxensor) in HEK-293 cells stably transfected with SLC9B2	10.5281/zenodo.7360521
K562	IC₅₀	41 μM Compound: Phloretin	Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay	[PMID: 24775915]
MCF7	IC₅₀	> 10 μM Compound: 5b	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 26690274]
MCF7	IC₅₀	7 μM Compound: Phloretin	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 6 days by SRB assay	[PMID: 33257172]
MDA-MB-231	IC₅₀	> 10 μM Compound: 5b	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 26690274]
NCI-H1299	IC₅₀	54 μM Compound: Phloretin	Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human H1299 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 24200808]
Vero	IC₅₀	125 μg/mL Compound: 31	Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 22169259]
Vero	CC₅₀	735.47 μg/mL Compound: 31	Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells assessed as cell death after 72 hrs by MTT assay	[PMID: 22169259]

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.

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.

60-82-2

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

Microorganisms

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
10 mM	0.3646 mL	1.8230 mL	3.6460 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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μL

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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

Purity: 99.67%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (245 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Kasahara T, Kasahara M. Expression of the rat GLUT1 glucose transporter in the yeast Saccharomyces cerevisiae. Biochem J. 1996 Apr 1;315 ( Pt 1):177-82. [Content Brief]

[2]. Luo H, et al. Phloretin induces apoptosis of BEL-7402 cells in vitro. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Jul;28(7):1249-51. [Content Brief]

[3]. Huang WC, 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 Oct;57(10):1803-13. [Content Brief]

[4]. Wang SP, et al. Potent Antiarthritic Properties of Phloretin in Murine Collagen-Induced Arthritis.Evid Based Complement Alternat Med. 2016;2016:9831263. [Content Brief]

Complete Stock Solution Preparation Table

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

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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Phloretin (Synonyms: NSC 407292; RJC 02792)

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Phloretin Related Antibodies

16 Publications Citing Use of MCE Phloretin

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View All GLUT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Phloretin Related Antibodies

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Complete Stock Solution Preparation Table

Phloretin Related Classifications

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