Cat. No.: HY-N0143A

Phlorizin dihydrate

(Synonyms: Floridzin dihydrate)

17 Cited Publications

Customer Review

Based on 17 publication(s) in Google Scholar

Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

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

Purity: 98.0%
CAS No.: 7061-54-3
Formula: C₂₁H₂₈O₁₂
Molecular Weight:472.44

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Phlorizin dihydrate Chemical Structure

CAS No.: 7061-54-3

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (17)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]^[4]

hSGLT1

0.04 μM (IC₅₀)

hSGLT1

39 nM (Ki)

hSGLT2

0.17 μM (IC₅₀)

hSGLT2

0.31 nM (Ki)

JAK2

STAT3

Caspase-3

Caspase-7

All SGLT Isoforms :

SGLT1
SGLT2

All PI3K Isoforms :

All Akt Isoforms :

All GLUT Isoforms :

All NF-κB Isoforms :

All JAK Isoforms :

All STAT Isoforms :

All Caspase Isoforms :

All DNA/RNA Synthesis Isoforms :

All mTOR Isoforms :

In Vitro

Phlorizin (30 min) dihydrate, a competitive inhibitor, potently inhibits sodium-dependent AMG transport in COS-7 cells expressing wild-type mSGLT2, with a mean K_i of 65 nM and a mean IC₅₀ of 0.07 μM^[1].
Phlorizin (10 min) dihydrate shows significantly reduced inhibitory potency against sodium-dependent AMG transport in COS-7 cells expressing the hSGLT1^C610K mutant, with a mean IC₅₀ of 1.7 μM, which is 10-fold higher than that of wild-type hSGLT1^[1].
Phlorizin (30 min) dihydrate significantly enhances the inhibitory potency against sodium-dependent AMG transport in COS-7 cells expressing the hSGLT2^C615K mutant, with a mean IC₅₀ of 0.017 μM, which is 2-fold lower than that of wild-type hSGLT2^[1].
Phlorizin (30 min) dihydrate significantly enhances the inhibitory potency against sodium-dependent AMG transport in COS-7 cells expressing the mSGLT2^N173A mutant, with a mean IC₅₀ of 0.018 μM^[1].
Phlorizin (1-100 μM) dihydrate inhibits glucose transport in renal tubular cells and intestinal cells^[2].
Phlorizin (100-150 μg/mL) dihydrate alleviates hydrogen peroxide-induced oxidative stress, DNA damage and apoptosis in human HepG2 cells by regulating the expression of Nrf2 protein and apoptosis-related genes^[4].
Phlorizin (6.25-100 μM) dihydrate inhibits Zika virus infection in cell models by reducing the activities of apoptotic caspase-3/-7, decreasing the phosphorylation level of the Akt/mTOR pathway, and lowering viral titers^[4].
Phlorizin dihydrate inhibits biofilm formation by up to 70% Staphylococcus aureus in RN4220 cells^[4].
Phlorizin dihydrate enhances the survival rate of human SH-SY5Y neuroblastoma cells and cerebral cortical neurons exposed to hydrogen peroxide or high-glucose environments by inhibiting SGLT-mediated Na⁺ and glucose influx^[4].
Phlorizin dihydrate exerts anti-tumor effects in human KYSE450 and KYSE30 esophageal cancer cells by inhibiting proliferation, invasion, migration and autophagy, and by activating apoptosis via antagonizing the JAK2/STAT3 signaling pathway^[4].

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

In Vivo

Phlorizin dihydrate normalizes insulin sensitivity in partially pancreatectomized diabetic rats by reducing blood glucose, while it has no effect on insulin action in control rats^[2].
Phlorizin (p.o.) dihydrate inhibits the increase in blood glucose levels in healthy mice following glucose loading^[2].
Phlorizin (p.o.) dihydrate leads to its complete conversion to Phloretin (HY-N0142) (90% as glucuronide or sulfate conjugates) in healthy rats, followed by excretion in urine^[2].
Phlorizin (through the interior of the proximal convoluted tubule) dihydrate into the proximal convoluted tubule impairs single-nephron glomerular filtration rate and renal tubular ion reabsorption function in streptozotocin-induced diabetic rats, but exerts no effect on normal control rats^[2].
Phlorizin (administered into the fourth ventricle) dihydrate increases feeding behavior in healthy rats^[2].
Phlorizin (intracerebroventricular administration; single dose) dihydrate induces FOS expression in periventricular glial cells of healthy rats and activates the transcriptional activity of multiple neurons in the central nervous system within 2 hours after administration^[2].
Phlorizin (1 mM, administered via endotracheal intubation) dihydrate reduces alveolar fluid absorption in healthy rats^[2].
Phlorizin dihydrate enhances memory in healthy rats and mice in passive avoidance tasks, and this effect is independent of blood glucose or cerebral glucose uptake^[2].
Phlorizin dihydrate enhances learning ability in healthy mice and blocks insulin-induced memory impairment when administered after learning^[2].
Phlorizin (chronic administration) dihydrate induces glycosuria, polyuria and weight loss in healthy dogs, mimicking the symptoms of human diabetes^[2].
Phlorizin (100 mg/kg; subcutaneous injection; once daily for 23 weeks) dihydrate adequately controls hyperglycemia in female obese SDT rats, completely prevents peripheral neuropathy and retinal/ocular complications, and partially reduces indicators associated with diabetic nephropathy^[3].
Phlorizin (20-40 mg/kg) dihydrate exerts antioxidant effects in D-Galactose (HY-N0210)-induced senescent mice by regulating the IL-1β/IκB-α/NF-κB signaling pathway; doses of 20 and 40 mg/kg increase the activity of antioxidant enzymes and reduce malondialdehyde levels^[4].
Phlorizin (6.25-25 mg/kg) dihydrate inhibits BVDV infection in mice at doses of 6.25, 12.5, and 25 mg/kg by regulating the levels of innate immune cytokines and pattern recognition receptors^[4].
Phlorizin (20 mg/kg) dihydrate improves blood glucose control and lipid metabolism in db/db type 2 diabetic mice, reduces levels of FBG, TC, TG and LDL-C, and increases HDL-C level^[4].
Phlorizin (30-120 mg/kg) dihydrate alleviates streptozotocin (STZ) (HY-13753)-induced diabetes in rats at doses of 30, 60, and 120 mg/kg by improving glycolipid metabolic profiles, protecting pancreatic islets, and regulating glycogen synthase kinase-3 and the ubiquitin-proteasome pathway^[4].
Phlorizin (200 mg/kg) dihydrate inhibits the JAK2/STAT3 signaling pathway in STZ-induced conscious diabetic rats at a dose of 200 mg/kg^[4].
Phlorizin (10 mg/kg) dihydrate exerts anti-tumor activity in HepG2 tumor xenograft mice by inhibiting PKC expression and regulating apoptosis^[4].
Phlorizin (1-5 μmol/200 μL) dihydrate blocks the ERK signaling pathway by inactivating NF-κB-induced COX-2 expression, thereby inhibiting TPA (HY-18739)-induced skin tumor formation in mice at doses of 1 and 5 μmol/200 μL^[4].
Phlorizin (0.4 g/kg) dihydrate restores glycemic control and ameliorates non-alcoholic steatohepatitis (NASH) in MSG (HY-W250122)-induced obese type 2 diabetic mice at a dose of 0.4 g/kg^[4].
Phlorizin dihydrate inhibits UVB-induced skin damage in nude mice by regulating the MAPK/NF-κB apoptotic signaling pathway^[4].
Phlorizin (intracerebroventricular administration) dihydrate reduces cerebral infarction volume in MCAO model mice via inhibition of SGLT and anti-apoptotic signaling pathways when administered intracerebroventricularly^[4].
Phlorizin dihydrate alleviates DSS (HY-116282C)-induced acute colitis in mice, reduces disease symptoms and improves intestinal morphology^[4].
Phlorizin (i.p.) dihydrate reduces BCAO-induced hippocampal cell death and improves learning/memory abilities in male ddY mice, and its mechanism of action may involve inhibiting the expression of SGLT family genes^[4].
Phlorizin dihydrate inhibits ischemic contracture and ischemia-induced arrhythmia in guinea pig myocardium by regulating voltage-dependent calcium channels and blocking Ca²⁺ influx^[4].

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

Animal Model:

SDT fatty (female, 6 weeks old at start, spontaneous obese type 2 diabetes with leptin receptor signaling defect)^[3]
Dosage:

100 mg/kg
Administration:

s.c.; once daily; 23 weeks
Result:

Controlled plasma glucose levels to a near-normal range throughout the experiment.
Reduced HbA1c levels to match normal control rats.
Delayed the age-related decrease in plasma insulin.
Significantly decreased urinary glucose excretion compared to vehicle-treated rats.
Had minimal effects on plasma triglyceride, free fatty acid, and total cholesterol levels.
Significantly decreased creatinine clearance.
Partially reduced urinary albumin excretion and urinary 8-OHdG levels.
Completely prevented Armanni-Ebstein changes, but did not reverse glomerulosclerosis, tubular regeneration, or interstitial inflammatory cell infiltration (and was associated with increased tubular dilation and urothelial inflammatory cell infiltration).
Corrected sciatic motor nerve conduction velocity (MNCV) to 95.6% of normal control levels and sciatic sensory nerve conduction velocity (SNCV) to 98.3% of normal control levels.
Prevented the decrease in intraepidermal nerve fiber density (IENFD) to 23.6 fibers/mm.
Significantly reduced prolongation of oscillatory potential peak latencies in electroretinograms.
Completely prevented retinal folding and thickening.
Prevented progression of cataracts.

Chemical Information

CAS No. 7061-54-3
Appearance Solid
Molecular Weight 472.44
Formula C₂₁H₂₈O₁₂
Color White to off-white
SMILES

O=C(C1=C(O)C=C(O)C=C1O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O)CCC3=CC=C(O)C=C3.O.O
Synonyms

Floridzin dihydrate
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

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Journal Impact Factor

Acta Pharm Sin B

Chrysin serves as a novel inhibitor of DGK α/FAK interaction to suppress the malignancy of esophageal squamous cell carcinoma (ESCC). [Abstract]

2021 Jan;11(1):143-155. PMID: 33532186
Carbohydr Polym

Oral absorption characteristics and mechanisms of a pectin-type polysaccharide from Smilax china L. across the intestinal epithelium. [Abstract]

2021 Oct 15:270:118383. PMID: 34364625
Nano Today

2024 Aug.
Food Chem

Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]

2025 Dec 30:497:146992. PMID: 41285060
Food Chem

Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]

2025 May 31:489:144992. PMID: 40466530
Phytomedicine

Protective effects of E Se tea extracts against alcoholic fatty liver disease induced by high fat/alcohol diet: In vivo biological evaluation and molecular docking study. [Abstract]

2022 Jul:101:154113. PMID: 35490493
Free Radic Biol Med

SGLT1 inhibition alleviates radiation-induced intestinal damage through promoting mitochondrial homeostasis. [Abstract]

2024 Nov 1:224:831-845. PMID: 39393555
Ind Crops Prod

2026 May 8;246:123392.
Ind Crops Prod

2025 Dec 11;239:122458.
Int Immunopharmacol

2026 May 27:184:116921. PMID: 42202394
Int Immunopharmacol

Phlorizin attenuates lupus nephritis via upregulating PI3K/Akt pathway-mediated Treg differentiation. [Abstract]

2025 Apr 4:154:114607. PMID: 40186900

Phlorizin dihydrate purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 4:154:114607. [Abstract]

Phlorizin (PHZ 40 mg/kg). Representative images of H&E and PAS staining in the kidneys of 22-week-old MRL/MpJ and MRL/lpr mice.

Phlorizin dihydrate purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 4:154:114607. [Abstract]

Phlorizin (PHZ 40mg/kg) treatment reduced the total urinary protein level in MRL/lpr mice.

Phlorizin dihydrate purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 4:154:114607. [Abstract]

Phlorizin (PHZ 40 mg/kg) administration led to an increase in the proportion of Treg cells. Flow cytometry analysis of representative CD25 and Foxp3 expression in CD4+ T cells under different treatment conditions was performed.

Phlorizin dihydrate purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 4:154:114607. [Abstract]

Phlorizin (PHZ 40 mg/kg) treatment promotes Treg cell development by activating the PI3K/Akt/FoxO1 pathway.

Phlorizin dihydrate purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2025 Apr 4:154:114607. [Abstract]

Western blot analysis of Phlorizin (PHZ 200 μM) showed that the expression of PI3K, p-PI3K, Akt, p-Akt, FoxO1 and Foxp3 all increased after treatment.
Bioorg Chem

Discovery of cyanidin-3-O-galactoside as a novel CNT2 inhibitor for the treatment of hyperuricemia. [Abstract]

2024 Dec 30:154:108108. PMID: 39753042
RSC Adv

Cytosolic β-glucosidase inhibition and renal blood flow suppression are leading causes for the enhanced systemic exposure of salidroside in hypoxic rats. [Abstract]

2018 Feb 23;8(16):8469-8483. PMID: 35539855
Virus Res

Decreased NHE3 activity and trafficking in TGEV-infected IPEC-J2 cells via the SGLT1-mediated P38 MAPK/AKt2 pathway. [Abstract]

2020 Apr 15;280:197901. PMID: 32070687
Biochem Biophys Res Commun

Glucose transports in the ileum: mechanism, regulation and physiological role of ileal glucose absorption. [Abstract]

2025 Sep 19:785:152676. PMID: 41005286
bioRxiv

2024 Mar 30.
SSRN

2023 Jun 15.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (211.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1167 mL

10.5834 mL

21.1667 mL

5 mM

0.4233 mL

2.1167 mL

4.2333 mL

10 mM

0.2117 mL

1.0583 mL

2.1167 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

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

Solubility: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.58 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (296 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pajor AM, et al. Inhibitor binding in the human renal low- and high-affinity Na+/glucose cotransporters. J Pharmacol Exp Ther. 2008;324(3):985-991. [Content Brief]

[2]. Chang WT, et al. Evaluation of the anti-inflammatory effects of phloretin and phlorizin in lipopolysaccharide-stimulated mouse macrophages. Food Chem. 2012;134(2):972-979. [Content Brief]

[3]. Katsuda Y, et al. Contribution of hyperglycemia on diabetic complications in obese type 2 diabetic SDT fatty rats: effects of SGLT inhibitor phlorizin. Exp Anim. 2015;64(2):161-169. [Content Brief]

[4]. Ni T, et al. Phlorizin, an Important Glucoside: Research Progress on Its Biological Activity and Mechanism. Molecules. 2024;29(3):741. Published 2024 Feb 5. [Content Brief]

[5]. Ehrenkranz JR, et al. Phlorizin: a review. Diabetes Metab Res Rev. 2005 Jan-Feb;21(1):31-8.
[Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1167 mL	10.5834 mL	21.1667 mL	52.9168 mL
	5 mM	0.4233 mL	2.1167 mL	4.2333 mL	10.5834 mL
	10 mM	0.2117 mL	1.0583 mL	2.1167 mL	5.2917 mL
	15 mM	0.1411 mL	0.7056 mL	1.4111 mL	3.5278 mL
	20 mM	0.1058 mL	0.5292 mL	1.0583 mL	2.6458 mL
	25 mM	0.0847 mL	0.4233 mL	0.8467 mL	2.1167 mL
	30 mM	0.0706 mL	0.3528 mL	0.7056 mL	1.7639 mL
	40 mM	0.0529 mL	0.2646 mL	0.5292 mL	1.3229 mL
	50 mM	0.0423 mL	0.2117 mL	0.4233 mL	1.0583 mL
	60 mM	0.0353 mL	0.1764 mL	0.3528 mL	0.8819 mL
	80 mM	0.0265 mL	0.1323 mL	0.2646 mL	0.6615 mL
	100 mM	0.0212 mL	0.1058 mL	0.2117 mL	0.5292 mL

Phlorizin dihydrate

17 Cited Publications

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Phlorizin dihydrate

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