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Varenicline (CP 526555, Chantix, Champix) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
| Molecular Weight | 284.18 |
| Formula | C13H15Cl2N3 |
| CAS Number | 866823-63-4 |
| Solubility (25°C) | DMSO 57 mg/mL Water 57 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
[4] A Tomillero, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
[5] M Bays, et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials
| Related AChR/AChE Products |
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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. |
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| 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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