AChR
Inhibitory Selectivity
Isoform-specific Inhibitors
AChR Products
Catalog No. | Information | Product Use Citations | Product Validations |
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S3245 |
NodakenetinNodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
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S9219 |
Huperzine BHuperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
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S5886 |
HodostinHodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis. |
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S3246 |
Picfeltarraenin IBPicfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation. |
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S3820 |
Dehydroevodiamine hydrochlorideDehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production. |
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S9252 |
CorydalineCorydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
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S0766 |
RHC 80267RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
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S9260 |
NodakeninNodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM. |
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S5022 |
Varenicline HydrochlorideVarenicline (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. |
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S3913 |
Pimethixene maleatePimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
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S3311 |
MyosmineMyosmine 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. |
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S9069 |
Jatrorrhizine chlorideJatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
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S3884 |
JatrorrhizineJatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
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S3904 |
IsoimperatorinIsoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM. |
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S9138 |
Picfeltarraenin IAPicfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system. |
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S0016 |
SN-6SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation. |
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S6985New |
VareniclineVarenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. |
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S0032 |
BatefenterolBatefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively. |
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S4713 |
AtropineAtropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
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S5777 |
Ipratropium bromide monohydrateIpratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
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S3298 |
Caulophylline (N-Methylcytisine)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. |
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S0717 |
Varenicline (CP 526555) dihydrochlorideVarenicline (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. |
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S0720 |
PNU-282987PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM. |
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E0176New |
DinotefuranDinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs. |
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E0172New |
ImidaclopridImidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity. |
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S7366 |
LY2119620LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
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S9789 |
JHU37152JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
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S9790 |
JHU37160JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
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S6887 |
Clozapine N-oxideClozapine N-oxide (CNO) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist. |
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S0457 |
DREADD agonist 21DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
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S6795 |
VU0357017 HydrochlorideVU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM. |
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S0552 |
BNC210BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
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S0782 |
VU0238441VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively. |
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S0783 |
VU0119498VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively. |
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S5931 |
BQCABQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
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S5844 |
Lobelin sulphateLobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation. |
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S2646 |
VU0238429VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4. |
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S4804 |
1-Naphthyl acetate1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S3245 |
NodakenetinNodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
||
S9219 |
Huperzine BHuperzine B, a natural alkaloid existed in Lycopodium plants, is a novel acetylcholinesterase inhibitor and has neuroprotective effects. |
||
S5886 |
HodostinHodostin (Neostigmine methyl sulfate, Syntostigmin, Neostigmeth) is a reversible inhibitor of acetylcholinesterase (AChE), but can not cross the blood-brain barrier. It is used in the treatment of myasthenia gravis. |
||
S3246 |
Picfeltarraenin IBPicfeltarraenin IB, a cucurbitacin glycoside isolated from Picriafel-terrae, is an inhibitor of acetylcholinesterase (AChE). Picfeltarraenin IB can be used for the treatment of herpes infections, cancer and inflammation. |
||
S3820 |
Dehydroevodiamine hydrochlorideDehydroevodiamine (DHE), a major phytochemical in fruits of Evodia rutaecarpa, can inhibit AChE. It has hypotensive and neuroprotective effects and modulates nitric oxide production. |
||
S9252 |
CorydalineCorydaline is a bioactive alkaloid with various anti-acetylcholinesterase, anti-allergic, and anti-nociceptive activities found in the medicinal herb Corydalis Tubers. |
||
S0766 |
RHC 80267RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
||
S9260 |
NodakeninNodakenin ((+)-Marmesinin), a coumarin compound, acts as an AChE inhibitor that inhibits AChE activity in a dosedependent manner with an IC50 value of 84.7 μM. |
||
S5022 |
Varenicline HydrochlorideVarenicline (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. |
||
S3913 |
Pimethixene maleatePimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively. |
||
S3311 |
MyosmineMyosmine 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. |
||
S9069 |
Jatrorrhizine chlorideJatrorrhizine chloride (Neprotine, Yatrorhizine) is the hydrochloride salt form of jatrorrhizine, which is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
||
S3884 |
JatrorrhizineJatrorrhizine (Neprotin, Yatrorizine), one of the active constituents of Coptis chinensis Franch, has multiple bioactivities, such as hypoglycemic, antimicrobial, and antioxidant activities. It is an inhibitor of AChE with IC50 of 872 nM and demonstrates >115-fold selectivity for AChE over BuChE. |
||
S3904 |
IsoimperatorinIsoimperatorin, a natural furanocoumarin that can be isolated from a variety of plant parts, has analgesic, antimicrobial, vascular relaxing and anticancer activities. Isoimperatorin is a methanolic extract of the roots of Angelica dahurica shows significant inhibitory effects on acetylcholinesterase (AChE) with the IC50 of 74.6 μM. |
||
S9138 |
Picfeltarraenin IAPicfeltarraenin IA is an AChE inhibitior, and an potential PI3K and EGFR inhibitor. It also acts as an inhibitor on both the classical and alternative pathways of the complement system. |
||
S0016 |
SN-6SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S6985New |
VareniclineVarenicline is highly selective and blocks more potently to α4β2 receptors than to other common nicotinic receptors (>500-fold α3β4, >3,500-fold α7, >20,000-fold α1βγδ), or to non-nicotinic receptors and transporters (>2,000-fold). Varenicline also acts as an agonist of 5-HT3 serotonine receptors. |
||
S0032 |
BatefenterolBatefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively. |
||
S4713 |
AtropineAtropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect. |
||
S5777 |
Ipratropium bromide monohydrateIpratropium bromide (Atrovent, Sch 1000) monohydrate is an antagonist of muscarinic acetylcholine receptors (mAChR) with IC50 of 2.9 nM, 2.0 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. |
||
S3298 |
Caulophylline (N-Methylcytisine)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. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S0717 |
Varenicline (CP 526555) dihydrochlorideVarenicline (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. |
||
S0720 |
PNU-282987PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM. |
||
E0176New |
DinotefuranDinotefuran (MTI-446), a neonicotinoid, is an effective nAChRs agonist with EC50 of 7.8 μM and shows high insecticidal activity on Da2b2 hybrid nAChRs. |
||
E0172New |
ImidaclopridImidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity. |
||
S7366 |
LY2119620LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors. |
||
S9789 |
JHU37152JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
||
S9790 |
JHU37160JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively. |
||
S6887 |
Clozapine N-oxideClozapine N-oxide (CNO) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist. |
||
S0457 |
DREADD agonist 21DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM. |
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S6795 |
VU0357017 HydrochlorideVU0357017 hydrochloride (CID-25010775) is a potent, highly selective and CNS-penetrant agonist of M1 which is a subtype of muscarinic acetylcholine receptors (mAChRs). VU0357017 hydrochloride appears to act at an allosteric site to activate the receptor with EC50 of 477 nM and Ki of 9.91 μM. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S0552 |
BNC210BNC210 (H-Ile-Trp-OH, IW-2143) is a negative allosteric modulator of alpha-7 nicotinic acetylcholine receptor (α7 nAChR). |
||
S0782 |
VU0238441VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50 of 2.1 μM, 2.2 μM, 2.8 μM, 3.2 μM and >10 μM for M5, M3, M2, M1 and M4, respectively. |
||
S0783 |
VU0119498VU0119498 is a pan Gq muscarinic acetylcholine receptor (mAChR) M1, M3, M5 positive allosteric modulator (PAM) with EC50 of 6.1 μM, 6.4 μM, 4.1 μM, respectively. |
||
S5931 |
BQCABQCA (benzylquinolone carboxylic acid) is a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR). |
||
S5844 |
Lobelin sulphateLobelin sulphate (Lobeline sulfate, Bantron) is an alkaloid that has actions similar to nicotine on nicotinic cholinergic receptors but is less potent. It has a variety of therapeutic uses including in respiratory disorders, peripheral vascular disorders, insomnia, and smoking cessation. |
||
S2646 |
VU0238429VU0238429 (M5 PAM) is the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5/M5) with EC50 of 1.16 μM at M5 and both > 30 μM at M1 and M3. VU0238429 shows no potentiator activity at M2 or M4. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S4804 |
1-Naphthyl acetate1-Naphthyl acetate is usually used in a rapid staining method for identification of macrophages. 1-Naphthyl acetate is a potent chromogenic substrate for the detection of erythrocyte acetylcholinesterase (AChE) activity. |