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 Experiment | |
|---|---|
| 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. |
| Concentrations | ~10 μM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 568.59 |
| Formula | C29H31F3N6O3 |
| CAS Number | 1421227-53-3 |
| Solubility (25°C) | DMSO: ≥ 60 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.
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