Phloretin (NSC 407292; RJC 02792) 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 (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. 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. 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.
Phloretin (50 or 100 mg/kg; oral administration; once daily) decreases oxidative stress and diminished levels of malondialdehyde (MDA) and hydrogen peroxide (H2O2) in paw tissue, reduces productivity of anti-collagen antibodies in serum.
Molecular Weight | 274.27 |
Formula | C15H14O5 |
CAS Number | 60-82-2 |
Solubility (25°C) | DMSO 45 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Talita Pizza Anunciato Casarini, et al. Dermatological applications of the flavonoid phloretin
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