mAChR 选择性抑制剂 | 激动剂 | 拮抗剂 | 调节剂

目录号 产品详情
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.

S5873

Scopolamine HBr trihydrate

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

S4713

Atropine

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

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.

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.

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).

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.

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.

S3144

Darifenacin HBr

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

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.

S0457

DREADD agonist 21

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

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.

S1913

Tropicamide

Tropicamide(Ro 1-7683) is an anticholinergic and a muscarinic receptor subtype M4-preferring antagonist with IC50 of 8.0 nM.

S2508

Scopolamine (LSM-4015) HBr

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

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.

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.

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.

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.

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.

S4027

Flavoxate HCl

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

S3047

Otilonium Bromide

Otilonium bromide is an antimuscarinic.

S1929

Irsogladine

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

S3735

Umeclidinium bromide

Umeclidinium bromide(GSK573719A) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD).

S3048

Solifenacin succinate

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

S2455

Bethanechol chloride

Bethanechol chloride(Myocholine,Urecholine) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.

S4292

Diphenidol HCl

Diphenidol HCl(Diphenidol hydrochloride) 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.

S4034

Diphemanil Methylsulfate

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

S2614

Arecoline HBr

Arecoline(NSC-31750) is a muscarinic acetylcholine receptor agonist.

S4231

Pilocarpine HCl

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

S1683

Ipratropium Bromide

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

S1978

Methscopolamine

Methscopolamine is a muscarinic acetylcholine receptor blocker.

S4143

Pentoxyverine Citrate

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

S3117

Oxybutynin hydrochloride

Oxybutynin(MJ4309-1) is an anticholinergic medication used to relieve urinary and bladder difficulties.