WS6 induced up to 4% of rat β cells to proliferate, with an EC50 of 0.4 μM. In the same format, WS6 also induced 3% of human β cells to proliferate, with a similar potency to the rat β cells. WS6 induced R7T1 proliferation in dose response, with EC50 value of 0.28 μM.
In vivo, WS6 (50 mg/kg p.o.) in RIP-DTA mouse model of β cell ablation ameliorates diabetes, and induces concomitant increases in β cell proliferation and β cell number.
|Cell lines||R7T1 cells|
|Preparation method||R7T1 cells are growth-arrested by removal of doxycycline for 2 days and plated into 384-well plates at a density of 3,000 cells/well in growth medium. Β cell proliferation is assessed using CellTiter Glo after 4 days. Fold increase in cell number is calculated by normalizing compound-treated wells to the median of DMSO-treated wells.|
|Incubation time||4 days|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 60 mg/mL|
Small-molecule inducer of β cell proliferation identified by high-throughput screening.
Shen W, et al. J Am Chem Soc. 2013 Feb 6;135(5):1669-72. PMID: 23330637.
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