BChE Inhibitor

CL-13 is a butyrylcholinesterase (BChE) inhibitor, with an IC₅₀ of 1.15 μM, and a selectivity index (SI) of 9.2 for acetylcholinesterase. CL-13 shows antioxidant activity in SH-SY5Y cells (DPPH EC₅₀ = 47.01 μM) and has the ability to chelate metals involved in Aβ aggregation and/or oxidative stress, showing no neurotoxicity at 50 μM. CL-13 can reverse cognitive impairment caused by scopolamine (HY-N0296) without affecting the mice's motor skills.

AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC₅₀s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ_1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease.

AChE/BChE-IN-24 (compound 5k) is a neuroprotective agent through cholinesterase inhibition. AChE/BChE-IN-24 inhibits AChE and BChE with IC₅₀ values of 16.38 μM and 10.44 μM, respectively.

hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC₅₀=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC₅₀=0.542 μM), and does not inhibit Dyrk1A (IC₅₀>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.

Lakoochin C is an inhibitor of acetylcholinesterase (AChE) (IC₅₀ = 61.86 μM) and butyrylcholinesterase (BChE) (IC₅₀ = 47.21 μM). Lakoochin C may be used in research related to Alzheimer's disease.

eeAChE-IN-3 (compound YS3g) is an orally active, potent EeAChE and IL-6 inhibitor with IC₅₀s of 0.54 μM, 0.49 μM, 8.54 μM and 0.57 μM for EeAChE, RatAChE, RatBuChE and IL-6, respectively. eeAChE-IN-3 improves STZ (HY-13753) (Streptozotocin; HY-13753)-induced learning and memory impairment in mice. eeAChE-IN-3 has the potential for Alzheimer's disease (AD) research.

BChE-IN-26 (Compound 7b) is a selective AChE and BChE inhibitor with K_i value of 35 μM and 1.6 μM. BChE-IN-26 has cytotoxicity to human neuroblastoma (SH-SY5Y) cell line. BChE-IN-26 can be used for the research of Alzheimer’s disease.

α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC₅₀ of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC₅₀ of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models.

2-Methyl-2-butenyl (E)-Caffeate is a type of caffeic acid ester compound. The petroleum ether and chloroform extracts containing 2-Methyl-2-butenyl (E)-Caffeate have inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The ether extract containing 2-Methyl-2-butenyl (E)-Caffeate exhibits strong antioxidant properties. 2-Methyl-2-butenyl (E)-Caffeate can be used in the research of Alzheimer's disease.

AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC₅₀ of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro.

AChE-IN-67 (compound 8n) is a potent AChE inhibitor, with an IC₅₀ of 0.033 μM. AChE-IN-67 exhibits activity similar to Donepezil (HY-14566). AChE-IN-67 exhibits high blood-brain barrier (BBB) permeability. AChE-IN-67 can be used for Alzheimer's disease research.

AChE/BChE-IN-26 (Compound 20aa) is a cholinesterase inhibitor with IC₅₀ values of 0.75 μM and 4.11 μM against eeAChE and eqBChE, respectively. AChE/BChE-IN-26 has antioxidant activity and can be used in the research of diseases such as Alzheimer's disease.

AChE/BuChE-IN-6 (Compound 11f) is an inhibitor of AChE and BuChE, with IC₅₀ values of 1.24 and 1.85 μg/mL, respectively. AChE/BuChE-IN-6 also exhibits strong DPPH free radical scavenging activity (IC₅₀ = 3.15 μg/mL). In vivo toxicity studies indicate that AChE/BuChE-IN-6 is safe, showing no significant differences in blood and biochemical markers compared to the control group after long-term administration, and no abnormalities were observed in liver and kidney tissues. AChE/BuChE-IN-6 holds promise for research into Alzheimer's disease.

Monogynol A is an AChE/BChE inhibitor found in the aerial parts of Salvia trichoclada Bentham. Monogynol A can be used for the research of alzheimer’s disease.

COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC₅₀ of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC₅₀ values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB.

BChE-IN-15 (Compound 6) is a pseudo-irreversible and covalent BChE inhibitor with an IC₅₀ of 1.76 nM against hBChE .

LINS05414 is a histamine H3 receptor ligand with antiCholinesterase and metal chelating activities. LINS05414 exhibits inhibitory activity against acetylcholinesterase (pIC₅₀ = 4.03) and butyrylcholinesterase (pIC₅₀ = 3.83), with a pK_i of 6.37 for human histamine H3 receptors. LINS05414 chelates copper ions, ferrous ions and ferric ions. LINS05414 regulates the release of neurotransmitters. LINS05414 can be used in the research of neurodegenerative diseases.

Multi-kinase-IN-13 (Compound 10F) is an inhibitor of AChE, BuChE, and GSK-3β, with an IC₅₀ of 3 nM against hAChE, 303 nM against hBuChE, and 7.58 nM against GSK-3β. Multi-kinase-IN-13 exhibits in vitro iron chelating activity. AChE-IN-110 can be used in the research of Alzheimer's disease.

AChE-IN-102 (compound C8) is a potent, selective and competitive AChE inhibitor with a K_i of 7.55 nM and an IC₅₀ of 15.25 nM. AChE-IN-102 shows selectivity over BuChE (IC₅₀ = 21.15 nM, b>K_i = 6.17 nM). AChE-IN-102 can be used for Alzheimer’s disease research.

(+)-(3S)-ψ-Ribalinine is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with an IC₅₀ of 62.46 μM against electric eel acetylcholinesterase and an IC₅₀ of 150.04 μM against equine butyrylcholinesterase. (+)-(3S)-ψ-Ribalinine can be used for the research of neurological disorders.