1. Membrane Transporter/Ion Channel Neuronal Signaling
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  3. TC-2559

TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a Ki value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases.

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TC-2559

TC-2559 Chemical Structure

CAS No. : 326924-19-0

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Description

TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a Ki value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases[1].

In Vitro

TC-2559 binds with high affinity to nicotinic acetylcholine receptors in rat brain cortex membranes, with a Ki of 5.5 nM[1].
TC-2559 (0.01-100 μM) potently and efficaciously stimulates dopamine release from rat striatal synaptosomes (EC50 = 203 nM) and induces significantly less residual inhibition of dopamine release than nicotine following pre-incubation[1].
TC-2559 (0.01-90 μM) potently stimulates 86Rb+ efflux from rat thalamic synaptosomes, with an EC50 of 367 nM and efficacy comparable to nicotine[1].
TC-2559 (10 μM; 2 h) significantly protects cultured fetal rat brain cells from glutamate-induced neurotoxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TC-2559 (3-6 μmol/kg; subcutaneous injection; single administration) significantly reverses scopolamine-induced cognitive impairment in male Sprague-Dawley rats in the step-through passive avoidance test[1].
TC-2559 (1-10 μmol/kg; p.o.; single administration or daily administration for 6 consecutive days) enhances radial arm maze working memory performance in male Sprague-Dawley rats (acute administration), improves their reference memory at an acute dose of 1 μmol/kg, and repeated oral administration (1-6 μmol/kg) further enhances their working memory performance[1].
TC-2559 (1-10 μmol/kg; subcutaneous injection; single administration) induces dose-dependent hypoactivity in male Sprague-Dawley rats. A dose of 1 μmol/kg produces a persistent effect, and both 1 μmol/kg and 10 μmol/kg doses significantly reduce locomotor activity over 30 minutes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 200-350 g, scopolamine-induced amnesia)[1]
Dosage: 0.6 μmol/kg; 1 μmol/kg; 3 μmol/kg; 6 μmol/kg; 10 μmol/kg
Administration: s.c.; single dose
Result: Significantly attenuated scopolamine-induced reduction in step-through retention latencies at 3 μmol/kg (median latency 88.7 s) and 6 μmol/kg (median latency 105.7 s).
Did not produce statistically significant attenuation at 0.6 μmol/kg, 1 μmol/kg, and 10 μmol/kg compared to scopolamine alone.
Molecular Weight

311.30

Formula

C12H18N2O·1/2C6H10O8

CAS No.
SMILES

OC([C@@H](O)[C@H](O)[C@H](O)[C@@H](O)C(O)=O)=O.CNCC/C=C/C1=CN=CC(OCC)=C1.[1/2]

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TC-2559
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HY-183204
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