AChE Inhibitor

AChE-IN-8 (Compound 19) is a potent inhibitor of AChE with an IC₅₀ of 1.95 μM. AChE-IN-8 has the potential for the research of Alzheimer's disease.

CUR-IPA is a cholinesterase inhibitor, with IC₅₀ of 5.99, 59.30, and 60.66 μM for eAChE (electric eel), hAChE (human), and hBChE (human), respectively. CUR-IPA can scavenge free radicals and has antioxidant activity. CUR-IPA can be used in the research of cognitive dysfunction.

AChE/BChE-IN-25 (Compound 6e) is the orally active inhibitor for hAChE and eqBChE with IC₅₀ of 7.9 nM and 0.79 nM. AChE/BChE-IN-25 exhibits antioxidant activity, that scavenges free radical with IC₅₀ of 22.91 μM. AChE/BChE-IN-25 exhibits neuroprotective effects by reducing mitochondrial and cellular oxidative stress in the Drosophila Alzheimer's disease model. AChE/BChE-IN-25 ameliorates Scopolamine (HY-N0296)-induced spatial and cognitive memory impairment in mouse model.

AChE/BChE-IN-27 is a blood-brain barrier-permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC₅₀ values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC₅₀ value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD).

AChE-IN-46 (compound 4), a β-cyclocostunolide, is an AChE inhibitor.

Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC₅₀ values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research.

AChE/BChE-IN-33 (Compound 3N) is a dual-target inhibitor of AChE and BChE, with IC₅₀ values of 12.81 and 44.54 nM respectively. AChE/BChE-IN-33 exhibits selective cytotoxicity against SH-SY5Y cells. AChE/BChE-IN-33 can be used for the study of Alzheimer's disease and neuroblastoma.

AChE-IN-114 is a selective AChE inhibitor and shows weak inhibitory activity for BChE. AChE-IN-114 can be used for the research of alzheimer’s disease.

Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC₅₀ values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).

Trimethylammonium chloride-¹³C₃,d₉ is the ¹³C₃,d₉-labeled Trimethylammonium chloride (HY-Y0504). Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.

Trimethylammonium chloride-d₁₀ (Hegzadesil-d₁₀) is the d₁₀-labeled Trimethylammonium chloride (HY-Y0504). Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.

AChE-IN-17 (compound 1) is a potent AChE inhibitor with an IC₅₀ value of 28.98 μM. AChE-IN-17 can significantly prevent H₂O₂-induced PC12 cell death, exhibiting excellent neuroprotective effect. AChE-IN-17 can be used for researching neurodegenerative diseases (NDs).

AChE/BuChE-IN-8 is a dual AChE and BuChE inhibitor, with an AChE IC₅₀ of 1.18 μM, a human AChE K_i of 1.2 μM, and a BuChE IC₅₀ of 2.34 μM. AChE/BuChE-IN-8 acts as an antiproliferative agent and antioxidant, exerts antiproliferative effects on colon cancer cells, scavenges free radicals, and exhibits reducing power. AChE/BuChE-IN-8 can be used in the research of Alzheimer's disease and colorectal adenocarcinoma.

CEase-IN-1 (Compound A1H3) is a potent and selective cholesterol esterase (CEase) inhibitor with an IC₅₀ of 0.36 μM. CEase-IN-1 can be used for the research of hypercholesterolemia.

AChE-IN-93 (compound 4m) is a potent AchE inhibitor with an IC₅₀ of 29 nM. AChE-IN-93 can be used in Alzheimer's disease research.

Trimethylammonium chloride-¹⁵N (Hegzadesil-¹⁵N) is the ¹⁵N-labeled Trimethylammonium chloride (HY-Y0504). Trimethylammonium chloride (Hegzadesil) is a non-competitive Acetylcholinesterase inhibitor. Trimethylammonium chloride reversibly blocks the deacetylation of acetylcholinesterase.

AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT_1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC₅₀ value 2.29 nM against AChE, EC₅₀ value 58.6 nM against 5-HT_1A and IC₅₀ value against SERT. Orally active.

ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ_1-42 aggregation inhibitor with IC₅₀s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ_1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent.

MPQPPAK is a polypeptide obtained from the enzymatic hydrolysis of C-phycocyanin (HY-D1025) and possesses neuroprotective activity. MPQPPAK enhances the activities of antioxidant enzymes SOD, CAT, and GSH-Px, reduces ROS, inhibits apoptosis and acetylcholinesterase (AChE) activity in brain tissue, and decreases protein carbonyl content. In the MPTP (HY-W114750)-induced zebrafish Parkinson's disease model, MPQPPAK exhibits antioxidant effects, inhibits autophagy and apoptosis, reverses the loss of dopaminergic neurons and cerebral blood vessels, and alleviates motor deficits. MPQPPAK can be used for research on Parkinson's disease.

NSS-18 is a potent and reversible inhibitor of AChE and MAO-B, with IC₅₀ values of 1.53 and 1.51 μM respectively. NSS-18 can inhibit the self-aggregation of Aβ. NSS-18 inhibits the intracellular generation of ROS induced by Aβ. NSS-18 shows a moderate neuroprotective effect against 6-OHDA (HY-B1081)-induced neurotoxicity. NSS-18 can form chelates with metal ions such as Cu²⁺, Fe³⁺, and Zn²⁺, with the strongest chelation being with Cu²⁺. NSS-18 can be used for the study of Alzheimer's disease.