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Hesperetin

Cat. No. M1556
Hesperetin Structure
Synonym:

Hesperitin

Size Price Availability Quantity
50mg USD 46  USD46 In stock
100mg USD 80  USD80 In stock
200mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

Hesperetin is a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin exhibits strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC50 and Ki values lower than 10 µM) and moderately inhibits UGT1A4, UGT1A7, UGT1A8 (IC50 values 29.68-63.87 µM). Hesperetin dose-dependently reduces GCDCA-induced caspase-3 activity in cultured primary rat hepatocytes. Hesperetin also dose-dependently reduces CM-induced Nos2 (iNOS) expression in hepatocytes.

Hesperetin (200 mg/kg) attenuates Con A-induced hepatocyte apoptosis and hepatic Nos2 (iNOS) expression in mice. Hesperetin co-treatment also decreases the occurrence of apoptotic bodies, hydropic degeneration, nuclear fragments, autolysis and haemorrhage. The number of leukocytes infiltrated in liver tissue of mice with D-GalN/LPS-induced fulminant hepatitis are significantly decreased by hesperetin in a murine model.

Chemical Information
Molecular Weight 302.28
Formula C16H14O6
CAS Number 520-33-2
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage 4°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Li Q, et al. Nutr Cancer. Hesperetin Induces Apoptosis in Human Glioblastoma Cells via p38 MAPK Activation.

[2] Arya A, et al. Mater Sci Eng C Mater Biol Appl. Bioflavonoid hesperetin overcome bicalutamide induced toxicity by co-delivery in novel SNEDDS formulations: Optimization, in vivo evaluation and uptake mechanism.

[3] Liu D, et al. Biol Pharm Bull. Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb-Dr ug Interactions.

[4] Bai X, et al. Br J Pharmacol. The protective effect of the natural compound hesperetin against fulminant hepatitis in vivo and in vitro.

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Keywords: Hesperetin, Hesperitin supplier, p38 MAPK, inhibitors, activators


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