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Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor, it has potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM).
Zanapezil has a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil also inhibits ligand binding at alpha-1, alpha-2 and serotonin 2 receptors with Ki values of 324, 2330 and 3510 nM, respectively.
Zanapezil (3 mg/kg; oral administration) significantly accelerated the turnover rates of dopamine, noradrenaline and serotonin in the rat brain. Zanapezil (1~10 mg/kg; oral administration) induces a statistically significant and dose-dependent decrease in AChE activity in the cerebral cortex in ex vivo experiments.
| Molecular Weight | 376.53 |
| Formula | C25H32N2O |
| CAS Number | 142852-50-4 |
| Solubility (25°C) | DMSO 6 mg/mL |
| Storage | -20°C, protect from light |
| Related AChR/AChE Products |
|---|
| AT 1001
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) with Ki of 2.64 nM. |
| Dihydro-β-erythroidine hydrobromide
Dihydro-β-erythroidine hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. |
| Spinosad
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. |
| TAE-1
TAE-1 is a potent inhibitor of AChE and BuChE. |
| PE154
PE154 is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively). |
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