| Bioactivity | Tacrine hydrochloride is a potent inhibitor of both AChE and BChE, with IC50s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC50 of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease[1][2]. |
| Target | IC50: 31 nM (AChE), 25.6 nM (BChE), 26 μM (NMDAR) |
| Invitro | Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner[1].Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC50of ~500 μM[2].Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC50 of ~190 μM at -60 mV[2]. |
| In Vivo | Tacrine (20-40 μmol/kg; s.c.) disrupts retention of learning in 17- and 30-day old mice in passive avoidance, and while the low dose of tacrine treatment (5 μmol/kg; s.c.) improves retention in 17-day old mice[2].Tacrine (0.1-0.4 mg/mL; i.p. for 7 d) inhibits the expression of AChE, but does not significantly improve the protection of the retina function and morphology in mice[3]. |
| Name | Tacrine hydrochloride |
| CAS | 1684-40-8 |
| Formula | C13H15ClN2 |
| Molar Mass | 234.72 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Ahmed M, et, al. Inhibition of two different cholinesterases by tacrine. Chem Biol Interact. 2006 Aug 25; 162(2):165-71.c [2]. Horak M, et, al. The pharmacology of tacrine at N-methyl-d-aspartate receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2017 Apr 3;75: 54-62. [3]. The protective role of tacrine and donepezil in the retina of acetylcholinesterase knockout mice. Yi YM, et, al. Int J Ophthalmol. 2015 Oct 18; 8(5): 884-90. |