XEN445 is a potent and selective EL inhibitor (IC50=0.237 uM) which shows good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.XEN445 can be readily prepared in good yield from commercial available chemicals, which is selected for further evaluation of this series of EL inhibitors.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male EL knockout mice and age-matched wild-type male C57BL6 mice |
| Formulation | Suspended in 0.2% Tween-20/1% carboxymethyl-cellulose |
| Dosages | 30 mg/kg bid |
| Administration | p.o. |
| Molecular Weight | 366.33 |
| Formula | C18H17F3N2O3 |
| CAS Number | 1515856-92-4 |
| Solubility (25°C) | DMSO |
| 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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