Cetilistat is highly lipophilic, which facilitated their dissolution in the GTL without the need of a vehicle. Although cetilistat is a benzoxazinone lipase inhibitor, orlistat reacts with the nucleophilic serine of lipases via its β-lactone moiety, resulting in a covalent complex.
| Cell Experiment | |
|---|---|
| Cell lines | acinar cells |
| Preparation method | Pancreatic acini were harvested and preincubated with 50 μmol/L orlistat or cetilistat, after which linoleic acid (LA) or GTL was added, followed by incubation for 4 hours. |
| Concentrations | 50 μmol/L |
| Incubation time | 4 h |
| Animal Experiment | |
|---|---|
| Animal models | Wistar rats |
| Formulation | GTL |
| Dosages | 25 mg/mL |
| Administration | i.v. |
| Molecular Weight | 401.58 |
| Formula | C25H39NO3 |
| CAS Number | 282526-98-1 |
| Solubility (25°C) | 10 mM in 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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