BTS 54-505 hydrochloride is a potently active primary amine metabolite of sibutramine, exhibits a similar pharmacological profile to the parent compound. Inhibits serotonin and noradrenalin reuptake more potently than sibutramine in vitro. Reduces food intake in rodents following i.c.v. administration and increases energy expenditure via thermogenesis in vivo.
| Molecular Weight | 288.26 |
| Formula | C15H22NCl.HCl |
| CAS Number | 84484-78-6 |
| Solubility (25°C) | DMSO 28.83 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.
[1] Bain, et al. Biochem J. The specificities of protein kinase inhibitors: an update.
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