mAChR Selective Inhibitors | Agonists | Antagonists | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5258 Revefenacin

Revefenacin (TD-4208, GSK-1160724) is a potent, lung-selective, long-acting muscarinic antagonist that may be for the treatment of respiratory disease.

Selective
S4031 Aclidinium Bromide

Aclidinium Bromide (LAS 34273, LAS-W 330) inhibits human muscarinic AChR M1, M2, M3, M4 and M5 with Ki of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM, respectively.

Selective M5 mAChR, Ki: 0.16 nM; M4 mAChR, Ki: 0.21 nM; M3 mAChR, Ki: 0.14 nM; M2 mAChR, Ki: 0.14 nM; M1 mAChR, Ki: 0.1 nM
S9790 JHU37160

JHU37160 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.

Selective hM4Di, EC50: 0.2 nM; hM3Dq, EC50: 18.5 nM; hM4Di, Ki: 3.6 nM; hM3Dq, Ki: 1.9 nM
S5385 Imidafenacin

Imidafenacin (KRP-197, ONO-8025) is a urinary antispasmodic of the anticholinergic class. It is a novel antimuscarinic agent with safety and efficacy, has been clinically used for the treatment of overactive bladder. Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM). IC50 value: 0.3 nM(M3).

Selective M2 receptor, IC50: 4.13 nM; M3 receptor, Kd: 0.317 nM; M3 receptor, IC50: 0.3 nM
S3913 Pimethixene maleate

Pimethixene (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.

Selective Muscarinic M2, pKi: 9.38; Muscarinic M1, pKi: 8.61
S9789 JHU37152

JHU37152 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.

Selective hM4Di, EC50: 0.5 nM; hM3Dq, EC50: 5 nM; hM4Di, Ki: 8.7 nM; hM3Dq, Ki: 1.8 nM
S2659 5-hydroxymethyl Tolterodine (PNU 200577, 5-HMT, 5-HM)

5-hydroxymethyl tolterodine (PNU 200577) is a new muscarinic receptor antagonist with Kb of 0.84 nM.

Selective mAChR, Kb: 0.84 nM
S3144 Darifenacin HBr

Darifenacin HBr (UK-88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

Selective M3 mAChR, pKi: 8.9
S0032 Batefenterol 

Batefenterol (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.

Selective hM3 muscarinic receptor, Ki: 1.3 nM; hM2 muscarinic receptor, Ki: 1.4 nM
S5921 Cyclopentolate Hydrochloride

Cyclopentolate is an antagonist of muscarinic acetylcholine receptors with Ki values of 1.62, 27.5, and 2.63 nM for M1, M2, and M3 receptors, respectively.

Selective M3 receptor, Ki: 2.63 nM; M2 receptor, Ki: 27.5 nM; M1 receptor, Ki: 1.62 nM
S0457 DREADD agonist 21

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (hM3Dq) with EC50 of 1.7 nM.

Selective hM3Dq, EC50: 1.7 nM
S5777 Ipratropium bromide monohydrate

Ipratropium 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.

Selective M3 receptor, IC50: 1.7 nM; M2 receptor, IC50: 2.0 nM; M1 receptor, IC50: 2.9 nM
S2130 Atropine sulfate monohydrate

Atropine sulfate monohydrate is a competitive antagonist for the muscarinic acetylcholine receptor, used to decrease the production of saliva and secretions of the airway prior to surgery.

Selective mAChR, IC50: 2.5 nM
S1913 Tropicamide

Tropicamide is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.

Selective M4 mAChR, IC50: 8 nM
S2508 Scopolamine (LSM-4015) HBr

Scopolamine HBr (LSM-4015, NSC 61806) is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.

Selective mAChR, IC50: 55.3 nM
S4024 Homatropine Methylbromide

Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.

Selective mAChR (SHR-E), IC50: 170.3 nM; mAChR (WKY-E), IC50: 162.5 nM
S4025 Homatropine Bromide

Homatropine Bromide is an muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.

Selective mAChR (SHR-E), IC50: 170.3 nM; mAChR (WKY-E), IC50: 162.5 nM
S6795 VU0357017 Hydrochloride

VU0357017 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.

Selective M1 mAChR, Ki: 9.91 μM; M1 mAChR, EC50: 477 nM
S2646 VU0238429

VU0238429 (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.

Selective M3 mAChR, : ; M1 mAChR, : ; M5 mAChR, IC50: 1.16 μM
S0782 VU0238441

VU0238441 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.

Selective mAChR M4, IC50: >10 μM; mAChR M1, IC50: 3.2 μM; mAChR M2, IC50: 2.8 μM; mAChR M3, IC50: 2.2 μM; mAChR M5, IC50: 2.1 μM
S0783 VU0119498

VU0119498 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.

Selective mAChR M5, IC50: 4.1 μM; mAChR M3, IC50: 6.4 μM; mAChR M1, IC50: 6.1 μM
S4027 Flavoxate HCl

Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM.

Selective mAChR, IC50: 12.2 μM
S3735 Umeclidinium bromide

Umeclidinium bromide is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).

Selective
S2614 Arecoline HBr

Arecoline is a muscarinic acetylcholine receptor agonist.

Selective
S2455 Bethanechol chloride

Bethanechol chloride is a selective muscarinic receptor agonist without any effect on nicotinic receptors.

Selective
S3047 Otilonium Bromide

Otilonium bromide is an antimuscarinic.

Selective
S4231 Pilocarpine HCl

Pilocarpine HCl (NSC 5746) is a nonselective muscarinic acetylcholine receptor agonist used to produce an experimental model of epilepsy.

Selective
S4034 Diphemanil Methylsulfate

Diphemanil Methylsulfate is a quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors (mAchR).

Selective
S1929 Irsogladine

Irsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.

Selective
S3048 Solifenacin succinate

Solifenacin succinate (YM905) is a urinary antispasmodic of the antimuscarinic class.

Selective
S1683 Ipratropium Bromide

Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).

Selective
S1978 Methscopolamine

Methscopolamine is a muscarinic acetylcholine receptor blocker.

Selective
S4713 Atropine

Atropine (Atropen, Atnaa, Tropine tropate, DL-Hyoscyamine) is a competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.

Selective
S4292 Diphenidol HCl

Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02, respectively, used in the treatment of vomiting and vertigo.

Selective
S5873 Scopolamine HBr trihydrate

Scopolamine HBr is a competitive muscarinic acetylcholine receptor antagonist with an IC50 of 55.3 nM.

Selective
S3117 Oxybutynin hydrochloride

Oxybutynin is an anticholinergic medication used to relieve urinary and bladder difficulties.

Selective
S4143 Pentoxyverine Citrate

Pentoxyverine Citrate (Carbetapentane) is an antitussive (cough suppressant) commonly used for cough associated with illnesses like common cold.

Selective