Search Result

Results for "

M1 agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (13) Adrenergic Receptor (10) Akt (1) Amyloid-β (2) Androgen Receptor (2) Apoptosis (6) Autophagy (2) Bacterial (2) Calcium Channel (3) Cholinesterase (ChE) (1) Dopamine Receptor (5) Dopamine Transporter (4) Drug Derivative (1) Drug Isomer (1) Drug Metabolite (7) ERK (5) FXR (2) G protein-coupled Bile Acid Receptor 1 (3) GSK-3 (1) Histamine Receptor (4) iGluR (2) IKK (1) Influenza Virus (2) Interleukin Related (2) Isotope-Labeled Compounds (5) Ligands for E3 Ligase (1) mAChR (94) MARCKS (2) MyD88 (1) NF-κB (2) NO Synthase (1) Opioid Receptor (6) Orphan GPCR (1) p38 MAPK (3) PACAP Receptor (1) PI3K (1) PKA (1) Potassium Channel (4) PPAR (2) PROTACs (1) Protein Arginine Deiminase (1) Reference Standards (16) ROR (3) Serotonin Transporter (4) Sigma Receptor (3) Sodium Channel (4) Tau Protein (1) TNF Receptor (2) Toll-like Receptor (TLR) (2) Trk Receptor (4) Virus Protease (4)
By Research Areas:	Cancer (20) Cardiovascular Disease (3) Endocrinology (4) Infection (7) Inflammation/Immunology (17) Metabolic Disease (5) Neurological Disease (87)
Click Chemistry:	Alkynes (2)

111

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14539

Clozapine Maximum Cited Publications 11 Publications Verification HF 1854; ZINC000019796155	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor Ligands for E3 Ligase	Neurological Disease Cancer
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-105182

Xanomeline 5+ Cited Publications LY-246708	mAChR	Neurological Disease
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

HY-70020B

Cevimeline hydrochloride 2 Publications Verification AF102B hydrochloride	mAChR	Neurological Disease Cancer
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride can cross the blood-brain barrier (BBB) .

HY-105182A

Xanomeline tartrate 5+ Cited Publications LY 246708 tartrate	mAChR	Neurological Disease
Xanomeline (LY 246708) is the potent agonist of muscarinic *M1/M4* receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia .

HY-B0406A

Bethanechol chloride 2 Publications Verification Carbamyl-β-methylcholine chloride	mAChR	Neurological Disease Cancer
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .

HY-32067

Aceclidine Quinuclidin-3-yl acetate	mAChR	Cardiovascular Disease Neurological Disease
Aceclidine (Quinuclidin-3-yl acetate) is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC₅₀: 40 μM). Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .

HY-143712

Allolithocholic acid 1 Publications Verification	Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR	Metabolic Disease Inflammation/Immunology Cancer
Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

HY-G0021

N-Desmethylclozapine Norclozapine; Desmethylclozapine; Normethylclozapine	mAChR Opioid Receptor Drug Metabolite Virus Protease	Infection
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .

HY-15618

MK-7622 M1 receptor modulator	mAChR Calcium Channel	Neurological Disease
MK-7622 (M1 receptor modulator) is an orally active positive allosteric modulator of muscarinic M1 acetylcholine receptors (mAChRs). MK-7622 enhances ACh-induced calcium flux in CHO cells expressing human M1 receptors (EC₅₀ = 21 nM) and shows robust agonist activity in rat M1-expressing CHO cells, increasing intracellular calcium. MK-7622 reverses Scopolamine (HY-N0296)-induced cognitive deficits in rhesus macaques in an object retrieval detour task. MK-7622 can be used for the study of Alzheimer's disease (AD) .

HY-19752A

VU0357017 hydrochloride CID-25010775	mAChR	Neurological Disease
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M₁ muscarinic acetylcholine receptor, with an EC₅₀ of 477 nM. VU0357017 hydrochloride is highly selective for M₁ and has no activity at M₂-M₅ up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia .

HY-76772

Cevimeline hydrochloride hemihydrate 2 Publications Verification SNI-2011; AF102B hydrochloride hemihydrate	mAChR	Neurological Disease Cancer
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB) .

HY-70020

Cevimeline 2 Publications Verification AF102B	mAChR	Neurological Disease Cancer
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia . Cevimeline can cross the blood-brain barrier (BBB) .

HY-32067A

Aceclidine hydrochloride Quinuclidin-3-yl acetate hydrochloride	mAChR	Neurological Disease
Aceclidine (Quinuclidin-3-yl acetate) hydrochloride is a modulator of M3 muscarinic acetylcholine receptor and a M1 receptor agonist (EC₅₀: 40 μM). Aceclidine hydrochloride is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine hydrochloride has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia .

HY-101341

RS 67333 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pK_i of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .

HY-159829

Direclidine NBI-1117568; HTL-0016878	mAChR	Neurological Disease
Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .

HY-107111

GSK1034702	mAChR	Neurological Disease
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-176710

PAD-PF2	Protein Arginine Deiminase Opioid Receptor mAChR	Neurological Disease Inflammation/Immunology Cancer
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC₅₀ = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC₅₀ = 12.3 μM). The IC₅₀ values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca ²⁺-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .

HY-N7043

Isosilybin A 2 Publications Verification	Apoptosis PPAR NF-κB p38 MAPK ERK Androgen Receptor	Inflammation/Immunology Cancer
Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity ^[1][2][3].

HY-14562

TBPB	mAChR Amyloid-β	Neurological Disease Inflammation/Immunology
TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC₅₀=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis) .

HY-B1404

Nylidrin hydrochloride Buphenine hydrochloride	iGluR Influenza Virus	Infection Cardiovascular Disease Inflammation/Immunology
Nylidrin hydrochloride (Buphenine hydrochloride) is an orally active β-adrenergic agonist. Nylidrin hydrochloride antagonizes NR1_A/2B NMDA receptors (IC₅₀ = 0.18 μM in Xenopus oocytes). Nylidrin hydrochloride reduces the levels of NP, HA, and M1. Nylidrin hydrochloride has antiviral activity against multiple H1N1 subtype influenza A viruses. Nylidrin hydrochloride improves hemorrhagic shock and anti-allergic effects .

HY-116480

LY593093	mAChR	Neurological Disease
LY593093 is a selective, orally active, and brain-penetrant muscarinic M1 receptor agonist with an EC₅₀ of 22.8 nM. LY593093 can be utilized in Alzheimer’s disease research .

HY-100336

AC260584 1 Publications Verification	mAChR	Neurological Disease
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC₅₀ of 7.6.

HY-118363

Lu AE51090	mAChR	Neurological Disease
Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC₅₀ of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS) .

HY-128855

Talsaclidine	mAChR	Neurological Disease
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-113616A

VU0364572 TFA	MARCKS mAChR	Neurological Disease
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC₅₀ of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant .

HY-14539A

Clozapine hydrochloride Maximum Cited Publications 11 Publications Verification HF 1854 hydrochloride	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-116586

AF710B	Sigma Receptor mAChR ERK Amyloid-β Tau Protein	Neurological Disease
AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .

HY-14539R

Clozapine (Standard) Maximum Cited Publications 11 Publications Verification HF 1854 (Standard)	Reference Standards Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

HY-101586

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

HY-B0406

Bethanechol Carbamyl-β-methylcholine	mAChR	Neurological Disease Cancer
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .

HY-105182S1

Xanomeline-d3 LY-246708-d₃	Isotope-Labeled Compounds mAChR	Neurological Disease
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

HY-116586A

(Rac)-AF710B	mAChR Sigma Receptor	Neurological Disease
(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease .

HY-113970A

Nebracetam hydrochloride WEB 1881 FU hydrochloride	mAChR Calcium Channel	Neurological Disease
Nebracetam (WEB 1881 FU) hydrochloride is an orally active M₁ muscarinic receptor agonist. Nebracetam hydrochloride can induce an increase in intracellular Ca ²⁺ concentration, with an EC₅₀ value of 1.59 mM. Nebracetam hydrochloride exhibits neuroprotective activity and the ability to improve cognitive impairment. Nebracetam hydrochloride can be used in the research of neurological diseases such as Alzheimer's disease .

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-N4157

Isopteropodine	mAChR 5-HT Receptor Bacterial	Neurological Disease
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and 5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-123852

PF-06764427	mAChR	Neurological Disease
PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia .

HY-118806A

AC-42 hydrochloride	mAChR	Neurological Disease
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC₅₀s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .

HY-W014208

NGX-267 AF-267B	mAChR	Others
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .

HY-G0021S1

N-Desmethylclozapine-d8 hydrochloride Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride	mAChR Opioid Receptor Drug Metabolite Virus Protease	Infection
N-Desmethylclozapine-d₈ (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .

HY-120004

PF-06827443	mAChR	Infection
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .

HY-177410

*Muscarinic M1 receptor agonist-1*	mAChR	Neurological Disease
Muscarinic M1 receptor agonist-1 (Ex.1-21) is a Muscarinic M1 receptor agonist. Muscarinic M1 receptor agonist-1 can be used in the research of psychiatric disorders such as schizophrenia .

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-179047

SMU-L11-R	Toll-like Receptor (TLR) MyD88 IKK p38 MAPK ERK TNF Receptor Interleukin Related	Inflammation/Immunology Cancer
SMU-L11-R is a selective TLR7 agonist with an EC₅₀ of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 ⁺T cells. SMU-L11-R shows potential in colorectal cancer studies .

HY-U00038

ENS-163 phosphate ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate	mAChR	Neurological Disease
ENS-163 phosphate is a selective muscarinic M1 receptor agonist.

HY-149702

*M1/M4 muscarinic agonist* 1**	mAChR	Neurological Disease
M1/M4 muscarinic agonist 1 (compound 41) is a selective muscarinic M4/M1 agonist with EC₅₀ values of 14 and 55 nM for M4 and M1, respectively. M1/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusional disorder, etc .

HY-G0021S

N-Desmethylclozapine-d8 Norclozapine-d₈; Desmethylclozapine-d₈; Normethylclozapine-d₈	mAChR Opioid Receptor Drug Metabolite Virus Protease	Infection
N-Desmethylclozapine-d₈ is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .

HY-106432

Sabcomeline SB-202026; Memric	mAChR	Neurological Disease
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .

HY-116459

trans-Cevimeline hydrochloride AF102A hydrochloride	mAChR	Neurological Disease
Trans-Cevimeline (AF102A) (hydrochloride), as a trans-isomer of AF102B, is a M1 selective cholinergic agonist. Trans-Cevimeline (AF102A) (hydrochloride) can be used for the research of Alzheimer's disease .

HY-149732

*M1/M4 muscarinic agonist* 3**	mAChR	Neurological Disease
M1/M4 muscarinic agonist 3 (compound 44) is a muscarinic mAChR M1/M4 agonist with EC₅₀s of 31 nM and 9.3 nM, respectively .

HY-149703

*M1/M4 muscarinic agonist* 2**	mAChR	Neurological Disease
M1/M4 muscarinic antagonist 2 (compound 40) is a selective M1 and M4 agonist with IC₅₀19 nM and 42 nM, respectively .

Cat. No.	Product Name	Target	Research Area

HY-P6292

KS-133	PACAP Receptor PKA ERK PI3K Akt GSK-3	Neurological Disease Cancer
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-143712

Allolithocholic acid 1 Publications Verification	Structural Classification Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Steroids Source Classification	Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR
Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

HY-N7043

Isosilybin A 2 Publications Verification	Flavanonols Flavonoids Glycine soya Classification of Application Fields Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Disease Research Fields Source Classification Cancer	Apoptosis PPAR NF-κB p38 MAPK ERK Androgen Receptor
Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity ^[1][2][3].

HY-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and 5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-N7043R

Isosilybin A (Standard)	Flavanonols Structural Classification Flavonoids Glycine soya Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Source Classification	Reference Standards Apoptosis PPAR NF-κB p38 MAPK ERK Androgen Receptor
Isosilybin A (Standard) is the analytical standard of Isosilybin A (HY-N7043). Isosilybin A is a PPARγ agonist that can be isolated from silymarin. Isosilybin A activates extrinsic and intrinsic pathways of apoptosis through targeting of the Akt-NF-kB-AR axis. Isosilybin A can relieve the inflammatory response in the rosacea model via inhibiting Erk and p38 signaling pathways and M1 macrophage polarization, with its targets related to RELA and VEGFA. Isosilybin A has anti-prostate cancer (PCA) activity ^[1][2][3].

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and 5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-143712R

Allolithocholic acid (Standard)	Structural Classification Endogenous metabolite Steroids Source Classification	Reference Standards Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR
Allolithocholic acid (Standard) is the analytical standard of Allolithocholic acid (HY-143712). This product is intended for research and analytical applications. Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

Cat. No.	Product Name	Chemical Structure

HY-105182S1

Xanomeline-d3
Xanomeline-d₃ (LY-246708-d₃) is deuterium labeled Xanomeline. Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia .

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

HY-G0021S1

N-Desmethylclozapine-d8 hydrochloride

N-Desmethylclozapine-d₈ (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .

HY-G0021S

N-Desmethylclozapine-d8

N-Desmethylclozapine-d₈ is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .

HY-B0406AS

Bethanechol-d6 chloride
Bethanechol-d₆ (chloride) is the deuterium labeled Bethanechol chloride. Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system .

HY-143712S1

Allolithocholic Acid-d4

Allolithocholic Acid-d₄ (3α-hydoxy-5α-Cholaoic Acid-d₄, allo-LCA-d₄) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC₅₀ = 2.7 μM) and RORγt inverse agonist (IC₅₀ = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .

HY-14539S3

Clozapine-d3

Clozapine-d₃ (HF 1854-d₃) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM) .

Cat. No.	Product Name		Classification

HY-128855

Talsaclidine		Alkynes
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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 .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks