Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, high selectivity over other key metabolic lipases. Atglistatin inhibits lipolysis in cell and organ cultures by targeting ATGL with no cytotoxicity up to a concentration of 50 μM. In vivo, Atglistatin (i.p.) results in Dose and time-dependent inhibition of lipolysis. Oral treatment of Atglistatin causes a dose-dependent decrease in FA and glycerol of up to 50% and 62%, respectively. It also causes a strong reduction in plasma TG levels (43%). Atglistatin is selective for ATGL and reduces fatty acid mobilization both in vitro and in vivo.
| Molecular Weight | 283.37 |
| Formula | C17H21N3O |
| CAS Number | 1469924-27-3 |
| Solubility (25°C) | DMSO 47 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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