| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| ln Vitro |
In a concentration-dependent manner, tacrine (12.5-37.5 nM) inhibits both human blood butyrylcholinesterase and venom acetylcholinesterase [1]. With an IC50 of roughly 500 μM, tacrine lessens the neurotoxicity brought on by NMDAR activation in mouse cortical neuron cultures [2]. With an IC50 of roughly 190 μM at -60 mV, tacrine suppresses the NMDAR response in a concentration-dependent manner [2].
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|---|---|
| ln Vivo |
In mice aged 17 and 30, tacrine (20–40 μmol/kg; subcutaneous injection) reduces their ability to retain passive avoidance learning, but low-dose tacrine treatment (5 μmol/kg; subcutaneous injection) enhances their capacity to retain learning in 17-day-old mice [2]. Although tacrine (0.1–0.4 mg/mL; intraperitoneal injection for 7 days) can suppress AChE expression, its protective effects on mouse retinal morphology and function are not appreciably enhanced [3].
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| References | |
| Additional Infomation |
1,2,3,4-tetrahydro-9-aminoacridine hydrochloride monohydrate appears as yellow needles (from concentrated hydrochloric acid); white powder. pH of 1.5% solution: 4.5-6. Bitter taste. (NTP, 1992)
Tacrine Hydrochloride is the hydrochloride salt form of tacrine, an aminoacridine derivative with cognitive stimulating property. Although the mechanism of action has not been fully elucidated, tacrine hydrochloride may bind reversibly to cholinesterase, acetylcholinesterase as well as butyrylcholinesterase, thereby decreasing the breakdown of acetylcholine, and prolonging synaptic actions as well as increased release of acetylcholine. In addition, this agent inhibits monoamine oxidase (MAO) and may inhibit the reuptake of catecholamines and serotonin. Finally, a novel mechanism of action studied in animal models suggests tacrine to attenuate the production of interleukin-1beta in the hippocampus and blood, thereby producing central and peripheral anti-inflammatory effects that may play a role in Alzheimer's disease. A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. See also: Tacrine (has active moiety). |
| Molecular Formula |
C13H15CLN2
|
|---|---|
| Molecular Weight |
234.73
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| Exact Mass |
270.113
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| CAS # |
1684-40-8
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| Related CAS # |
Tacrine hydrochloride (hydrate);206658-92-6
|
| PubChem CID |
2723754
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| Appearance |
White to light yellow solid powder
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| Boiling Point |
409.4ºC at 760mmHg
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| Melting Point |
280-284 °C(lit.)
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| Flash Point |
230.5ºC
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| Vapour Pressure |
6.49E-07mmHg at 25°C
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| LogP |
4.079
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
16
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| Complexity |
229
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZUFVXZVXEJHHBN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H14N2.ClH/c14-13-9-5-1-3-7-11(9)15-12-8-4-2-6-10(12)13;/h1,3,5,7H,2,4,6,8H2,(H2,14,15);1H
|
| Chemical Name |
1,2,3,4-tetrahydroacridin-9-amine;hydrochloride
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| Synonyms |
NSC-72108; NSC72108; Hydroaminacrine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~33.33 mg/mL (~142.00 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 16.67 mg/mL (71.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2602 mL | 21.3011 mL | 42.6021 mL | |
| 5 mM | 0.8520 mL | 4.2602 mL | 8.5204 mL | |
| 10 mM | 0.4260 mL | 2.1301 mL | 4.2602 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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