Amyloid-β Inhibitor

Saikosaponin C (Standard) is the analytical standard of Saikosaponin C. This product is intended for research and analytical applications. Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.

RS-0466, a neuroprotective compound, inhibits β-amyloid-induced cytotoxicity. RS-0466 can be used for research of Alzheimer’s disease.

γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC₅₀ value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease.

hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE， MAO-B-IN-1 and BACE-1 inhibitor, with IC₅₀ values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease.

Ginsenoside Rg1 (Standard) is the analytical standard of Ginsenoside Rg1. This product is intended for research and analytical applications. Ginsenoside Rg1 is one of the major active components of Panax ginseng. Ginsenoside Rg1 ameliorates the impaired cognitive function, displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

3-O-Methyltolcapone-d₄ (Ro 40-7591 d₄) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC₅₀of 773 nM. Tolcapone can inhibits α-syn and Aβ₄₂ oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma.

AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC₅₀=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC₅₀= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research.

Ciliatoside A is a naturally bioactive compound that exhibits significant anti-inflammatory, antiviral, and neuroprotective activities. Ciliatoside A serves as a mitophagy inducer and NLRP3 inflammasome inhibitor, activating AMPK, SIRT1, and the PINK1/Parkin axis, and inhibiting pyroptosis and apoptosis. Ciliatoside A promotes autophagic flux, autophagosome-lysosome fusion, mTOR inhibition, and p62-dependent HBc degradation; reduces Aβ aggregation, plaque deposition, microglial/astrocyte activation, and bacterial load; and maintains neuronal integrity, mitochondrial membrane potential, and ATP production. Ciliatoside A is used in research on Alzheimer's disease, Klebsiella pneumoniae-induced pneumonia, hepatitis B virus infection, and inflammation.

(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

DEL-C1 is a CHI3L1 inhibitor. DEL-C1 can restore the ability to clear Amyloid-β and repair lysosomal function of astrocytes. DEL-C1 can inhibit NF-κB signaling and IL-6 secretion. DEL-C1 can be used for the researches of inflammation and neurological disease, such as Alzheimer's disease.

gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC₅₀ value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease.

Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC₅₀=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease.

SLAFVDVLN, a molecular peptide, is a BACE-1 inhibitor with a K_i value of 94 nM. SLAFVDVLN can reduce Aβ42 production.

TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC₅₀: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model.

RS-0406 is a beta-sheet breaker targeting Amyloid-β. RS-0406 can inhibits Aβ(1-42) fibrillogenesis and protect against Aβ(1-42)-induced cytotoxicity in primary hippocampal neurons. RS-0406 can be used for the research of neurological disease, such as Alzheimer's disease (AD).

BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC₅₀ values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research.

AChE/MAO-B-IN-9 (Compound E12) is an orally active, selective, reversible, non-competitive AChE and MAO-B inhibitor, with an IC₅₀ of 0.156 μM against electric eel AChE. AChE/MAO-B-IN-9 inhibits Aβ40/42 fibril formation, promotes Aβ fibril depolymerization, and inhibits Tau protein fibril formation. AChE/MAO-B-IN-9 exerts antioxidant and neuroprotective effects, and improves scopolamine (HY-N0296)-induced memory impairment in mice. AChE/MAO-B-IN-9 can be used for the research of Alzheimer's disease.

AChE-IN-88 (Compound 26) is a novel pyridazine derivative. AChE-IN-88 is an orally active multi-target ligand for Alzheimer's disease (AD) that inhibits both acetylcholinesterase (AChE) and amyloid β protein (Aβ) aggregation (pIC₅₀: 7.16).

BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC₅₀s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu²⁺, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s 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.