[CAS NO. 60-81-1] Phlorizin
PRODUCTS SPECIFICATIONS [60-81-1]
DESCRIPTION [60-81-1]
Overview
| MDL | MFCD00006591 |
|---|---|
| Molecular Weight | 436.41 |
| Molecular Formula | C21H24O10 |
| 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 |
5 Publications Citing Use of MCE
Summary
Phlorizin is a non-selective SGLT inhibitor with K i s of 300 and 39 nM for hSGLT1 and hSGLT2 , respectively. Phlorizin is also a Na + /K + -ATPase inhibitor.
IC50 & Target
|
SGLT1 |
SGLT2 |
In Vitro
Phlorizin is a non-selective SGLT inhibitor with K i s 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 PGE 2 levels. Phlorizin does not suppress IL-6 or TNF-α production, although 100 μM Phlorizin can significantly inhibit TNF-α expression [3] .
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Source
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
DMSO : ≥ 50 mg/mL ( 114.57 mM )
H 2 O : 1 mg/mL ( 2.29 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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 |
-
1.
Add each solvent one by one: 20% HP-β-CD in saline
Solubility: 15.15 mg/mL (34.72 mM); Clear solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution
-
5.
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
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.
- [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.
- [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.
- [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.
Synonyms