Tacrine hydrochloride (hydrate) is an inhibitor of both acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.
CAS Number | 206658-92-6 |
Solubility (25°C) | Water 90 mg/mL DMSO 32 mg/mL |
Storage | 2-8°C, dry, sealed |
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.
[3] Milena Sorrenti, et al. Solid-state characterization of tacrine hydrochloride
[4] Lauren T Bonner, et al. Pharmacologic treatments of dementia
[5] D Braida, et al. Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268)
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