Molecular Formula | C13H15ClN2 |
Molar Mass | 234.72 |
Melting Point | 280-284°C(lit.) |
Boling Point | 409.4°C at 760 mmHg |
Flash Point | 230.5°C |
Solubility | Soluble in aqueous buffers |
Vapor Presure | 6.49E-07mmHg at 25°C |
Appearance | Crystalline solid |
pKa | pKa 9.8 (Uncertain) |
Storage Condition | Inert atmosphere,2-8°C |
In vitro study | Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner. Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC 50 of ~500 μM. Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC 50 of ~190 μM at -60 mV. |
In vivo study | 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. 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. |
Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. R20/22 - Harmful by inhalation and if swallowed. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
UN IDs | UN 2811 6.1/PG 3 |
WGK Germany | 3 |
RTECS | AR9532500 |
Hazard Class | 6.1(a) |
Packing Group | II |
Toxicity | LD50 intravenous in mouse: 5600ug/kg |
EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
biological activity | Tacrine hydrochloride is an effective inhibitor of AChE and BChE, with IC50 values of 31 nM and 25.6 nM respectively. Tacrine hydrochloride is also an inhibitor of NMDAR with an IC50 value of 26 μM. Tacrine hydrochloride can be used to study Alzheimer's. |
Target | Value |
BChE (Cell-free assay) | 25.6 nM |
AChE (Cell-free assay) | 31 nM |