nAChR Selective Inhibitors | Agonists | Antagonists | Modulators
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
Varenicline (CP 526555) Hydrochloride is a potent and selective inhibitor of nicotine acetylcholine receptor (nAChR) with Ki of 0.12 nM and 0.14 nM for α6β2 nAChR and α4β2 nAChR, respectively.
|Selective||α4β2 nAChR, Ki: 0.14 nM; α6β2 nAChR, Ki: 0.12 nM|
Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
|Selective||α7 nAChR, Ki: 6.9 nM|
Benzethonium chloride is a potent inhibitor of nAChRs, it inhibits α4β2 nAChRs and α7 nAChRs with IC50 of 49 nM and 122 nM, respectively.
|Selective||α7 nAChRs, IC50: 122 nM; α4β2 nAChRs, IC50: 49 nM|
Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.
|Selective||nAChR, Kd: 50 nM|
PNU-120596 (Nsc 216666) is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.
|Selective||α7 nAChR, EC50: 216 nM|
Adiphenine HCl is a nicotinic receptor inhibitor, used as an antispasmodic drug.
|Selective||α4β4 nAChR, IC50: 6.3 μM; α4β2 nAChR, IC50: 3.7 μM; α3β4 nAChR, IC50: 1.8 μM; α1 nAChR, IC50: 1.9 μM|
|S0717||Varenicline (CP 526555) dihydrochloride||
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.
|Selective||α7 nAChRs, EC50: 18 μM; α3β4 nAChR, EC50: 55 μM; α4β2 nAChR, EC50: 2.3 μM|
Myosmine is not only one of the minor tobacco alkaloids but is also present in various foods. Myosmine has low affinity against a4b2 nicotinic acetylcholinergic receptors (nAChR) with Ki of 3300 nM.
|Selective||nAChR, Ki: 3300 nM|
|S4505||Vinblastine (NSC-49842) sulfate||
Vinblastine sulfate (NSC49842, Vincaleukoblastine sulfate salt, 29060-LE, Exal, Velban, Velbe) inhibits microtubule formation and suppresses nAChR activity with IC50 of 8.9 μM in a cell-free assay, used to treat certain kinds of cancer. Vinblastine sulfate induces autophagy and apoptosis.
|Selective||nAChR, IC50: 8.9 μM|
Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
|Selective||nAChR, IC50: 45.5 μM|
BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR).
Catharanthine inhibits nicotinic receptor mediated diaphragm contractions with IC50 of 59.6 μM.
|S4121||Succinylcholine Chloride Dihydrate||
Succinylcholine Chloride Dihydrate (Suxamethonium) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.
Cytisine (Baphitoxine, Sophorine) is a nicotinic acetylcholine receptor agonist.
Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
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