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M 2 Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (4) Adenosine Receptor (1) Adrenergic Receptor (4) Akt (2) Apoptosis (4) Autophagy (2) Calcium Channel (3) CaMK (2) Cholinesterase (ChE) (2) CRAC Channel (2) GnRH Receptor (1) Histamine Receptor (8) Isotope-Labeled Compounds (10) mAChR (79) mGluR (3) Na+/Ca2+ Exchanger (2) PACAP Receptor (1) PANoptosis (1) Parasite (2) PGC-1α (1) Phosphatase (1) Prostaglandin Receptor (1) Reference Standards (11) TRP Channel (2)
By Research Areas:	Cancer (14) Cardiovascular Disease (5) Endocrinology (7) Infection (1) Inflammation/Immunology (22) Metabolic Disease (10) Neurological Disease (62)
Click Chemistry:	Alkynes (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100001

SKF-96365 (hydrochloride) Maximum Cited Publications 27 Publications Verification	TRP Channel CRAC Channel Autophagy CaMK Akt Apoptosis Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-P6292A

KS-133 TFA	PACAP Receptor	Neurological Disease Inflammation/Immunology Cancer
KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC₅₀ values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation .

HY-A0034

Solifenacin 3 Publications Verification YM905 free base	mAChR	Neurological Disease Cancer
Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

HY-B0461

Trospium chloride	mAChR	Neurological Disease
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .

HY-A0030

Fesoterodine fumarate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-N0340

Scopolamine butylbromide 1 Publications Verification Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide	mAChR	Neurological Disease Inflammation/Immunology
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (K_i 83 nmol/L), hM2 (K_i 233 nmol/L), rat intestinal M3 (K_i 290 nmol/L) and hM3 (K_i 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .

HY-A0002

Solifenacin Succinate 3 Publications Verification YM905	mAChR	Neurological Disease Cancer
Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

HY-101381

Otenzepad 2 Publications Verification AF-DX 116	mAChR	Neurological Disease Metabolic Disease
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC₅₀ values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .

HY-B1339

Dicyclomine hydrochloride Dicycloverine hydrochloride	mAChR	Neurological Disease
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (K_i=5.1 nM) and M2 receptor subtype (K_i=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .

HY-107646

PD 102807	mAChR	Neurological Disease
PD 102807 is a M4 muscarinic receptor antagonist with an IC₅₀ of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC₅₀s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively . Antidyskinetic effect.

HY-107647

(S)-(+)-Dimethindene maleate 1 Publications Verification	mAChR Histamine Receptor	Inflammation/Immunology
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M₂-selective muscarinic receptor antagonist (pA₂ = 7.86/7.74; pK_i = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M₁ (pA₂ = 6.83/6.36; pK_i = 7.08), the M₃ (pA₂ = 6.92/6.96; pK_i = 6.70) and the M₄ receptors (pK_i = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H₁ receptor antagonist (pA₂ = 7.48) .

HY-70053

Fesoterodine	mAChR	Neurological Disease Metabolic Disease
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-B0241

Ipratropium bromide 1 Publications Verification Sch 1000	mAChR	Neurological Disease Inflammation/Immunology
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC₅₀s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .

HY-B1332

Ipratropium bromide hydrate 1 Publications Verification Sch 1000 bromide hydrate	mAChR	Neurological Disease Inflammation/Immunology
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC₅₀s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .

HY-116294A

Methoctramine tetrahydrochloride 1 Publications Verification	mAChR	Cardiovascular Disease
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine (HY-121404)-induced bradycardia in vivo. Methoctramine tetrahydrochloride can be used in the study of cardiovascular diseases .

HY-136587

Oxomemazine	Histamine Receptor mGluR	Inflammation/Immunology
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (K_i= 84 nM, M1 receptor) and low (K_i= 1.65 μM, M2 receptor) affinity sites. Oxomemazine is an antihistamine and anticholinergic agent used for the study of cough treatment. Oxomemazine is protective against anaphylactic microshock in guinea pigs .

HY-B1101A

Pimethixene maleate Pimetixene maleate	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .

HY-I0230

Solifenacin hydrochloride 3 Publications Verification YM905 hydrochloride	mAChR	Neurological Disease Cancer
Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

HY-122203

PCS1055 dihydrochloride 2 Publications Verification	mAChR Cholinesterase (ChE)	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively .

HY-B0461R

Trospium chloride (Standard)	mAChR Reference Standards	Neurological Disease
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .

HY-76570

(Rac)-5-Hydroxymethyl Tolterodine (Rac)-Desfesoterodine; (Rac)-PNU-200577	mAChR	Neurological Disease
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (K_i values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .

HY-14825A

Tarafenacin D-tartrate SVT-40776 D-tartrate	mAChR	Inflammation/Immunology
Tarafenacin (SVT-40776) D-tartrate is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin D-tartrate does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin D-tartrate can be used in the research of overactive bladder .

HY-101586

Alvameline Lu 25-109	mAChR	Neurological Disease
Alvameline (Lu25-109) is a partial M1 agonist and *M2/M3* antagonist.

HY-125942

SKF-96365 Maximum Cited Publications 27 Publications Verification	CRAC Channel TRP Channel CaMK Akt Apoptosis Autophagy Na+/Ca2+ Exchanger Calcium Channel	Neurological Disease Inflammation/Immunology Cancer
SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac I_Na/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G₂/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .

HY-B0461S

Trospium-d8 chloride	Isotope-Labeled Compounds mAChR	Neurological Disease
Trospium-d₈ (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .

HY-70053A

Fesoterodine L-mandelate	mAChR	Neurological Disease Metabolic Disease Cancer
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .

HY-148527

LAS190792 AZD8999	Adrenergic Receptor mAChR	Others
LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC₅₀ 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator .

HY-107656

PTAC oxalate	mAChR	Neurological Disease
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (K_i values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .

HY-A0030S

Fesoterodine-d7 fumarate	mAChR	Metabolic Disease
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-B1101

Pimethixene Pimetixene	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .

HY-151801

DIBA-Cy5	mAChR	Others
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the K_d value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .

HY-107653

J 104129 fumarate	mAChR	Neurological Disease
J 104129 fumarate is a selective and orally active muscarinic M3 antagonist with K_i values of 4.2 nM and 490 nM for M3 and M2, respectively. J 104129 fumarate antagonized ACh-induced bronchoconstriction. J 104129 fumarate has the potential for the research of obstructive airway disease .

HY-108171A

Hexocyclium methylsulfate	mAChR	Inflammation/Immunology
Hexocyclium methylsulfate is a potent mAChR antagonist with pK_i values of 8.9, 7.7, 8.4, 8.8 for M1, M2, M3, and M4 subtype, respectively. Hexocyclium methylsulfate has the potential for the research of duodenal ulcer and irritable bowel syndrome .

HY-U00302

CHF5407	mAChR	Inflammation/Immunology
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .

HY-P1376

*G-Protein antagonist* peptide**	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of G_i or G_o and inhibits G_s activation by β-adrenoceptors.

HY-101679A

YM-58790 free base	mAChR	Neurological Disease
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with K_i values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .

HY-100979

W-84 dibromide HDMPPA	mAChR	Others
W-84 (dibromide) is a potent allosteric modulator of *M2-cholinoceptors, which retards [ ³H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors* antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .

HY-107652

AF-DX 384	mAChR	Neurological Disease
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (K_is=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .

HY-B0241S

Ipratropium-d3 bromide Sch 1000-d₃	mAChR	Neurological Disease Inflammation/Immunology
Ipratropium-d₃ (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC₅₀ values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .

HY-B1339A

Dicyclomine Dicycloverine	mAChR	Neurological Disease
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (K_i=5.1 nM) and M2 receptor subtype (K_i=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .

HY-16375

Ozarelix D-63153	GnRH Receptor Apoptosis	Cancer
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .

HY-117087

K103	Phosphatase PANoptosis	Cancer
K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.

HY-123566

PSD-506 RO 3202904	mAChR	Metabolic Disease
PSD-506 (RO 3202904) is a muscarinic *M2/M3* antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence .

HY-171843

TD-6301	mAChR	Endocrinology
TD-6301 is a bladder-selective M_2/4 muscarinic receptor antagonist. TD-6301 binds to and blocks M_2/4 muscarinic receptors with high selectivity, especially human M₂ receptors with strong affinity (K_i = 0.36 nM). TD-6301 inhibits volume-induced bladder contractions (ID₅₀ = 0.075 mg/kg). TD-6301 can be used in the research of overactive bladder .

HY-U00104

YM-46303	mAChR	Endocrinology
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.

HY-129709

DAC 5945	mAChR	Cardiovascular Disease
DAC 5945 is a potent muscarinic antagonist in the airways than in the heart, with pK_i values of 8.3 and 7.52 for M1 and M2, respectively .

HY-P1376A

*G-Protein antagonist* peptide TFA** 1 Publications Verification	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

HY-169814

LU-25-077	mAChR	Neurological Disease
Lu 25-077 is a brain-penetrant and pharmacologically active N-demethyl metabolite of Lu 25-109 (HY-101586), a partial M1 agonist and *M2/M3* antagonist. Lu 25-077 can be utilized in neurological research .

HY-171449

SCH 211803	mAChR	Cardiovascular Disease Neurological Disease
SCH 211803 is a selective antagonist of the M₂ muscarinic receptor. SCH 211803 is promising for research of cardiovascular and nervous system diseases .

HY-122510

Atropine oxide Atropine oxidation	Parasite	Neurological Disease
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.

Cat. No.	Product Name	Target	Research Area

HY-P6292A

KS-133 TFA	PACAP Receptor	Neurological Disease Inflammation/Immunology Cancer
KS-133 TFA is a highly selective and potent antagonist of the vascular active enteropeptide receptor 2 (VIPR2) with IC₅₀ values for Ca influx measurement and cAMP measurement of 24.8 nM and 500 nM, respectively. KS-133 TFA reverses the tumor-promoting M2 phenotype of tumor-associated macrophages to the anti-tumor M1 phenotype, alters the tumor immune microenvironment, and inhibits tumor growth. KS-133 TFA can be used for research on schizophrenia and cancer immune regulation .

HY-P1376

*G-Protein antagonist* peptide**	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of G_i or G_o and inhibits G_s activation by β-adrenoceptors.

HY-16375

Ozarelix D-63153	GnRH Receptor Apoptosis	Cancer
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .

HY-P1376A

*G-Protein antagonist* peptide TFA** 1 Publications Verification	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0340

Scopolamine butylbromide 1 Publications Verification Hyoscine butylbromide; (-)-Scopolamine butylbromide; Butylscopolamine bromide	Alkaloids Structural Classification Other Alkaloids Datura metel L. Solanaceae Plants Source Classification	mAChR
Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (K_i 83 nmol/L), hM2 (K_i 233 nmol/L), rat intestinal M3 (K_i 290 nmol/L) and hM3 (K_i 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .

HY-N0340R

Scopolamine butylbromide (Standard) Hyoscine butylbromide (Standard); (-)-Scopolamine butylbromide (Standard); Butylscopolamine bromide (Standard)	Alkaloids Structural Classification Other Alkaloids Datura metel L. Solanaceae Plants Source Classification	Reference Standards mAChR
Scopolamine butylbromide (Standard) is the analytical standard of Scopolamine butylbromide (HY-N0340). This product is intended for research and analytical applications. Scopolamine butylbromide (Hyoscine butylbromide) is an orally active anticholinergic agent and spasmolytic. Scopolamine butylbromide binds with high affinity to rat cardiac M2 (K_i 83 nmol/L), hM2 (K_i 233 nmol/L), rat intestinal M3 (K_i 290 nmol/L) and hM3 (K_i 643 nmol/L) muscarinic receptors. Scopolamine butylbromide exerts a dose-dependent antagonistic effect on Carbachol-induced gastrointestinal smooth muscle spasm. Scopolamine butylbromide can be used for the research of abdominal colic and pain associated with gastrointestinal spasm, functional abdominal pain, chronic gastropathy and gastric ulcer .

Cat. No.	Product Name	Chemical Structure

HY-B0461S

Trospium-d8 chloride
Trospium-d₈ (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .

HY-A0030S

Fesoterodine-d7 fumarate
Fesoterodine-d₇ (fumarate) is the deuterium labeled Fesoterodine fumarate . Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .

HY-B0241S

Ipratropium-d3 bromide
Ipratropium-d₃ (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC₅₀ values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .

HY-I0230S

Solifenacin-d7 hydrochloride
Solifenacin-d₇ (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.

HY-A0002S

Solifenacin-d5 succinate
Solifenacin-d₅ (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.

HY-135329S

(1R,3S-)Solifenacin-d5 hydrochloride
(1R,3S-)Solifenacin-d₅ hydrochloride is the deuterium labeled Solifenacin hydrochloride. Solifenacin D₅ hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .

HY-70053S

rac-Fesoterodine-d14 fumarate
(Rac)-Fesoterodine-d₁₄ fumarate is a labelled racemic Fesoterodine. Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_ivalues of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-W720879

Fesoterodine-d3
Fesoterodine-d₃ is the deuterium labeled Fesoterodine (HY-70053). Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .

HY-B0241S1

Ipratropium-d7 bromide
Ipratropium-d₇ (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC₅₀ values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .

HY-76570S1

5-Hydroxymethyl Tolterodine-d14 formate

5-Hydroxymethyl Tolterodine-d₁₄ (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .

HY-76570S

(Rac)-5-Hydroxymethyl Tolterodine-d14

(Rac)-5-Hydroxymethyl Tolterodine-d₁₄ is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .

HY-B1339AS

Dicyclomine-d4

Dicyclomine-d₄ is the deuterium labeled Dicyclomine . Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .

HY-B1339S

Dicyclomine-d4 hydrochloride

Dicyclomine-d₄ hydrochloride (Dicycloverine-d₄ hydrochloride) is the deuterium labeled Dicyclomine hydrochloride (HY-B1339). Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .

Cat. No.	Product Name		Classification

HY-120329

Lu 26-046		Alkynes
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with K_i of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .

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