Phlorizin (Synonyms: Floridzin)

Name: Phlorizin
Brand: MedChemExpress
SKU: HY-N0143
Rating: 5.0 (9 reviews)

Cat. No.: HY-N0143 Purity: 99.93%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Phlorizin (Floridzin) is a non-selective SGLT inhibitor with K_is of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na⁺/K⁺-ATPase inhibitor.

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

Phlorizin Chemical Structure

CAS No. : 60-81-1

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Based on 9 publication(s) in Google Scholar

Other Forms of Phlorizin:

Phlorizin dihydrate Get quote
Phlorizin (Standard) Get quote

9 Publications Citing Use of MCE Phlorizin

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SGLT1 SGLT2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Phlorizin (Floridzin) is a non-selective SGLT inhibitor with K_is of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na⁺/K⁺-ATPase inhibitor.

IC₅₀ & Target

SGLT1

SGLT2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	108 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21128592]
CHO	IC₅₀	16 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins	[PMID: 21873071]
CHO	IC₅₀	16.4 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins	[PMID: 22889351]
CHO	IC₅₀	185 nM Compound: 1	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins	[PMID: 22889351]
CHO	IC₅₀	190 nM Compound: 1	Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins Inhibition of human SGLT1 expressed in CHO cells assessed as [14C]AMG uptake after 45 mins	[PMID: 21873071]
CHO	EC₅₀	197.4 nM Compound: 1	Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21128592]
CHO	IC₅₀	752 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake by fluorescence polarization assay	[PMID: 18755586]
CHO-K1	EC₅₀	0.077 μM Compound: 1	Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method	[PMID: 24071445]
CHO-K1	EC₅₀	0.12 μM Compound: 1	Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as inhibition of [14C]-AMG uptake up to 120 mins by scintillation counting method	[PMID: 24071445]
CHO-K1	EC₅₀	123 nM Compound: PZN	Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method Inhibition of human SGLT2 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method	[PMID: 27075813]
CHO-K1	EC₅₀	153 nM Compound: PZN	Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method Inhibition of human SGLT1 expressed in CHO-K1 cells assessed as reduction in [14C]AMG uptake after 120 mins by scintillation counting method	[PMID: 27075813]
CHO-K1	IC₅₀	16 nM Compound: Phlorizin	Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay	[PMID: 22652255]
CHO-K1	IC₅₀	190 nM Compound: Phlorizin	Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay	[PMID: 22652255]
COS-1	IC₅₀	0.1 mM Compound: Phlorizine	Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT2 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT2 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting	[PMID: 20189404]
COS-1	IC₅₀	0.2 mM Compound: Phlorizine	Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT1 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting Inhibition of alpha-D-[U-14C]glucopyranoside uptake at human SGLT1 expressed in african green monkey COS1 cells after 30 mins by liquid scintillation counting	[PMID: 20189404]
COS-7	IC₅₀	> 1000 μM Compound: phlorizin	Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method	[PMID: 25815140]
HEK293	IC₅₀	0.0673 μM Compound: 1	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	0.499 μM Compound: 1	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	58.6 nM Compound: Phlorizin	Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay Inhibition of SGLT2 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay	[PMID: 24556379]
HEK293	IC₅₀	60.7 nM Compound: Phlorizin	Inhibition of SGLT1 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay Inhibition of SGLT1 (unknown origin) expressed in HEK293 cells using 2-NBDG as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by nonradioactive fluorescence glucose uptake assay	[PMID: 24556379]
RAW264.7	IC₅₀	14.4 μM Compound: 14	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA	[PMID: 24679441]
RAW264.7	IC₅₀	14.6 μM Compound: 16	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA	[PMID: 31747281]

In Vitro

Phlorizin is a non-selective SGLT inhibitor with K_is of 300 and 39 nM for hSGLT1 and hSGLT2, respectively^[1]. Phlorizin is also a Na⁺/K⁺-ATPase inhibitor^[2]. Phlorizin at 2×10^-4 M inhibits Na⁺ and Rb⁺-activated ATPase activities in human red cell membranes by 43 %. At 1 mM and 7 mM RbCl, rubidium uptake is not changed or is slightly inhibited (less than 15 %) by 2×10^-4 M Phlorizin^[2]. Cell viability is not significantly altered by doses of Phlorizin <100 μM. Pretreating cells with Phlorizin does not significantly reduce nitrite or PGE₂ levels. Phlorizin does not suppress IL-6 or TNF-α production, although 100 μM Phlorizin can significantly inhibit TNF-α expression^[3].

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

In Vivo

Prior to Phlorizin treatment, the blood glucose level in SDT fatty rats is 370±49 mg/dL. Six hours after dosing, the blood glucose level in the Phlorizin treated group decreases to an almost normal level (139±32 mg/dL). Phlorizin-treated SDT fatty rats are heavier than vehicle-treated SDT fatty rats after 12 weeks. Phlorizin treatment significantly decreases glucose excretion and delays insulin decreases. Creatinine clearance decreases significantly with Phlorizin treatment. 23 weeks of Phlorizin treatment prevents the decrease of nerve fibers (23.6±3.2 fibers/mm). Retinal abnormalities are completely prevented with Phlorizin^[4].

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

Molecular Weight

436.41

Formula

C₂₁H₂₄O₁₀

CAS No.

60-81-1

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

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (114.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.29 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2914 mL	11.4571 mL	22.9142 mL
5 mM	0.4583 mL	2.2914 mL	4.5828 mL
10 mM	0.2291 mL	1.1457 mL	2.2914 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (5.73 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 (5.73 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 (5.73 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 1.75 mg/mL (4.01 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Protocol 2

Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 15.15 mg/mL (34.72 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.93%

Select Batch:

Data Sheet (290 KB) SDS (393 KB)

COA (262 KB) LCMS (93 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 Mar;324(3):985-91. [Content Brief]

[2]. Nakagawa A, et al. Localization of the phlorizin site on Na, K-ATPase in red cell membranes. J Biochem. 1977 May;81(5):1511-5. [Content Brief]

[3]. Chang WT, et al. Evaluation of the anti-inflammatory effects of phloretin and phlorizin in lipopolysaccharide-stimulated mouse macrophages. Food Chem. 2012 Sep 15;134(2):972-9. [Content Brief]

[4]. 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):161-9. [Content Brief]

Kinase Assay ^[1]	Resealed ghosts are obtained with the addition of 4×10^-3 M ATP and 5×10^-3 M MgCl₂ with or without 5×10^-4 M Phlorizin (final concentration) when red cells are hemolyzed. Ghosts corresponding to 0.4-0.45 mL of the original blood cells are incubated with 0.9 mL of Medium A and ⁸⁶RbCl for 45 or 90 min and the radioactivity in 200 μL of the supernatant is determined. The ATPase activity in the resealed ghosts is determined from the increase in inorganic phosphate after incubation^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	The RAW264.7 murine macrophage-derived cell line is used. Cell viability is measured using the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells (10⁵ cells/well) are cultured in 96-well plates and treated with varying concentrations of Phlorizin for 24 h. Next, the supernatant is removed and the cells are incubated with MTT (50 mg/mL) for 4 h at 37°C. The plates are washed and isopropanol is added to dissolve formazone crystals, then the absorbance values are measured at 570 nm using a microplate reader^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	Female SDT fatty rats are used in this study. At six weeks of age, SDT fatty rats are divided into two groups (n=8); a Phlorizin treated group and a vehicle treated group. Age-matched female Sprague-Dawley (SD) rats are used as control animals (n=8). Animals are housed in a climate-controlled room (temperature 23±3°C, humidity 55±15%, 12 h lighting cycle) and allowed free access to basal diet and water. Phlorizin is injected subcutaneously once daily (100 mg/kg/day) to animals in the Phlorizin treated group for 23 weeks. Twenty % propylene glycol is administered to animals in the vehicle treated group and control SD rats^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Pajor AM, et al. Inhibitor binding in the human renal low- and high-affinity Na+/glucose cotransporters. J Pharmacol Exp Ther. 2008 Mar;324(3):985-91. [Content Brief] [2]. Nakagawa A, et al. Localization of the phlorizin site on Na, K-ATPase in red cell membranes. J Biochem. 1977 May;81(5):1511-5. [Content Brief] [3]. Chang WT, et al. Evaluation of the anti-inflammatory effects of phloretin and phlorizin in lipopolysaccharide-stimulated mouse macrophages. Food Chem. 2012 Sep 15;134(2):972-9. [Content Brief] [4]. 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):161-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.2914 mL	11.4571 mL	22.9142 mL	57.2856 mL
DMSO	5 mM	0.4583 mL	2.2914 mL	4.5828 mL	11.4571 mL
	10 mM	0.2291 mL	1.1457 mL	2.2914 mL	5.7286 mL
	15 mM	0.1528 mL	0.7638 mL	1.5276 mL	3.8190 mL
	20 mM	0.1146 mL	0.5729 mL	1.1457 mL	2.8643 mL
	25 mM	0.0917 mL	0.4583 mL	0.9166 mL	2.2914 mL
	30 mM	0.0764 mL	0.3819 mL	0.7638 mL	1.9095 mL
	40 mM	0.0573 mL	0.2864 mL	0.5729 mL	1.4321 mL
	50 mM	0.0458 mL	0.2291 mL	0.4583 mL	1.1457 mL
	60 mM	0.0382 mL	0.1910 mL	0.3819 mL	0.9548 mL
	80 mM	0.0286 mL	0.1432 mL	0.2864 mL	0.7161 mL
	100 mM	0.0229 mL	0.1146 mL	0.2291 mL	0.5729 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Phlorizin Related Classifications

Metabolic Disease

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:

Phlorizin60-81-1FloridzinSGLTNa+/K+ ATPaseSodium-dependent glucose cotransportersSodium potassium pumpInhibitorinhibitorinhibit

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Phlorizin (Synonyms: Floridzin)

Customer Review

Other Forms of Phlorizin:

Phlorizin Related Antibodies

9 Publications Citing Use of MCE Phlorizin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All SGLT Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Phlorizin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Phlorizin Related Classifications

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