Resveratrol is a selective human cytochrome P450 1A1 inhibitor. Resveratrol slightly inhibited ethoxyresorufin O-deethylation (EROD) activity in human liver microsomes with an IC50 of 1.1 mM. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
Molecules. 2023 Apr 7.
Study of the Sensing Kinetics of G Protein-Coupled Estrogen Receptor Sensors for Common Estrogens and Estrogen Analogs
Resveratrol purchased from AbMole
|Cell lines||CNE-1 and CNE-2Z cells|
|Preparation method||Cell proliferation assay
The effect of resveratrol on the cell growth of CNE-1 and CNE-2Z cells was examined using the MTT assay. Cancer cells were plated in 96-well plates at 104 cells/well. Following pretreatment with different concentrations of resveratrol for 24 or 48 h, viable cells were determined using the MTT Assay kit (Chemicon, Temecula, CA, USA) according to the manufacturer’s protocol. At indicated time-points, 20 μl of MTT solution (5 mg/ml in PBS) were added into each well and incubated for 4 h. Then, 100 μl of DMSO was added to dissolve the crystals. The plate was then left to stand for 10 min at room temperature and the corresponding absorbance was measured at 490 nm. Each experiment was performed in triplicate.
|Concentrations||0, 10, 25, 50 and 100 μM|
|Incubation time||24 or 48 h|
|Animal models||female nude mice bearing CNE-2Z tumour xenograft model|
|Formulation||10% DMSO in PBS|
|Dosages||20 mg/kg once a day for 3 weeks|
|Solubility (25°C)||DMSO 46 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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