2. Membrane Transporter/Ion Channel PI3K/Akt/mTOR NF-κB Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis Cell Cycle/DNA Damage Anti-infection
  3. SGLT PI3K Akt GLUT NF-κB JAK STAT Caspase Apoptosis DNA/RNA Synthesis mTOR Bacterial
  4. Phlorizin dihydrate

Phlorizin dihydrate  (Synonyms: Floridzin dihydrate)

Cat. No.: HY-N0143A Purity: 98.0%
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Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki 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.

CAS No. : 7061-54-3

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10 mM * 1 mL in DMSO
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Based on 15 publication(s) in Google Scholar

Other Forms of Phlorizin dihydrate:

Phlorizin dihydrate Related Antibodies

Top Publications Citing Use of Products

    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.

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    Description

    Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki 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[1][2][3][4].

    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

     

    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 Ki 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 hSGLT1C610K 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 hSGLT2C615K 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 mSGLT2N173A 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.

    Phlorizin dihydrate Related Antibodies
    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.
    Molecular Weight

    472.44

    Formula

    C21H28O12
    CAS No.
    Appearance

    Solid

    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
    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
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1167 mL 10.5834 mL 21.1667 mL
    5 mM 0.4233 mL 2.1167 mL 4.2333 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, 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.

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 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.

      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: ≥ 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.

      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
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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: 99.51%

    SDS (393 KB)

    COA (261 KB) HNMR (124 KB) LCMS (244 KB)

    Handling Instructions (2659 KB)
    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, 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
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    Phlorizin dihydrate Related Classifications

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      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:

    Phlorizin dihydrate7061-54-3Floridzin dihydrateSGLTPI3KAktGLUTNF-κBJAKSTATCaspaseApoptosisDNA/RNA SynthesismTORBacterialSodium-dependent glucose cotransportersPhosphoinositide 3-kinasePKBProtein kinase BGlucose transporter Nuclear factor-κBNuclear factor-kappaBJanus kinaseMammalian target of RapamycinhSGLT1murine RAW264.7 macrophage-derived cellshuman SH-SY5Y neuroblastoma cellssodium-glucose cotransporter (SGLT)human HepG2 cellstype 2 diabetesCOS-7 cellshSGLT2mSGLT2Staphylococcus aureus RN4220 cellsInhibitorinhibitorinhibit

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