Amyloid-β Inhibitor

AChE-IN-59 (compounds 3b) is an AChE inhibitor, with an IC₅₀ value of 0.05 μM. AChE-IN-59 can inhibit the aggregation of Aβ1-42, protect nerve cells and penetrate the blood-brain barrier well. AChE-IN-59 can be used for the research of Alzheimer's disease (AD).

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

AP2238 is a dual-function acetylcholinesterase (AChE) inhibitor with K_i values for human AChE (HuAChE) and butyrylcholinesterase (BuChE) of 21.7 and 48.9 μM respectively. AP2238 blocks the pro-fibrotic interaction between the peripheral site of AChE and Aβ, and can inhibit Aβ aggregation. AP2238 can be used for the research of Alzheimer's disease.

Pyridoxal 5'-​phosphate (monohydrate) (Standard) is the analytical standard of Pyridoxal 5'-​phosphate (monohydrate). This product is intended for research and analytical applications. Pyridoxal 5'-phosphate monohydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate monohydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′-phosphate (PMP).

AD-35 is an orally active, blood-brain barrier-permeable acetylcholinesterase inhibitor with an IC₅₀ of 793 nM. AD-35 inhibits metal-induced amyloid-β aggregation and disassembles preformed amyloid-β aggregates. In rat models of cognitive impairment, AD-35 attenuates Aβ_25-35-induced astrocyte activation, TNF-α and IL-1β release, inhibits ERK phosphorylation, and alleviates learning and memory deficits. AD-35 can be used for research on Alzheimer's disease.

Glutaminyl Cyclase Inhibitor 6 (compound BI-43) is a secretory glutaminyl cyclase (sQC) and golgi-resident glutaminyl cyclase (gQC) inhibitor with IC₅₀ values of 0.012 0.040 µM, respectively. Glutaminyl Cyclase Inhibitor 6 has the potential for the research of Parkinson’s disease.

Pep63 is a neuroprotective peptide (VFQVRARTVA). Pep63 has a neuroprotective effect on synaptic plasticity and memory. Pep63 can competitively bind with Aβ1-42 oligomers, and can block Aβ fiber formation. Pep63 can be used for Alzheimer’s disease (AD) research.

Amyloid-β-IN-1 (compound 13) is a synthetic peptide containing the hydrophobic C-terminal region "VVIA-NH2" and its reverse sequence "AIVV-NH2" of Aβ₄₂, which is an Aβ inhibitor. Amyloid-β-IN-1 can inhibit Aβ aggregation and has neuroprotective effects.

20(S)-Ginsenoside Rg3 (Standard) is the analytical standard of 20(S)-Ginsenoside Rg3. This product is intended for research and analytical applications. 20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

Tolcapone (Standard) (Ro 40-7592 (Standard)) is the analytical standard 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/BChE-IN-21 is a histamine H₃ receptor antagonist, calcium channel blocker, and acetylcholinesterase inhibitor. AChE/BChE-IN-21 exhibits neuroprotective activity against H₂O₂ and Aβ_1-40, and can restore cognitive function in AD mice.

RI-OR2, a retro-inverso peptide, is an amyloid-β (Aβ) oligomerization inhibitor. RI-OR2 binds to immobilized β-Amyloid (1-42) (HY-P1363A) monomers and fibrils, with an apparent K_d of 9-12 μM, and also acted as an inhibitor of Aβ(1-42) fibril extension.

AChE/BChE-IN-37 is a blood-brain barrier-permeable AChE/BChE inhibitor, with an IC₅₀ of 73.65 μM against electric eel-derived AChE and an IC₅₀ of 82.93 μM against horse-derived BChE. AChE/BChE-IN-37 exhibits chelating activity towards Cu²⁺, Ca²⁺, Mg²⁺, Fe²⁺ and Zn²⁺. AChE/BChE-IN-37 interacts with HSP90AA1 and GSK-3β. AChE/BChE-IN-37 inhibits the self-induced aggregation of Aβ_1-42. AChE/BChE-IN-37 suppresses LPS-induced NO production in cells. AChE/BChE-IN-37 can be used in research related to Alzheimer's disease and inflammatory diseases.

AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC₅₀ values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC₅₀ of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB.

Anti-Aβ agent 1A (compound M15) has potent activity against amyloid-β. Anti-Aβ agent 1A possesses can significantly inhibit LPS-induced levels of IL-1β, IL-6 and TNF-α, and reduces the apoptosis of SH-SY5Y induced by H₂O₂ through mitochondria pathway. Anti-Aβ agent 1A possesses antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used for researching Alzheimer’s disease (AD).

Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC₅₀s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC_50hBACE-1=41.60 μM), amyloid β aggregation (IC_50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.

Keap1-Nrf2-IN-30 is an orally active, blood-brain barrier-permeable Keap1-Nrf2 protein-protein interaction inhibitor with a Keap1 K_d value of 157 nM. Keap1-Nrf2-IN-30 selectively inhibits the Keap1-Nrf2 protein-protein interaction, promotes Nrf2 nuclear translocation, suppresses induced ferroptosis, reduces the expression of Aβ and p-Tau, and upregulates the expression of GPX4 and SLC7A11. Keap1-Nrf2-IN-30 upregulates the expression of HO-1 and NQO1, alleviates neuronal damage, and improves cognitive and spatial memory deficits. Keap1-Nrf2-IN-30 can be used in the research of Alzheimer's disease.

RU-505 is an effective β-amyloid (Aβ)-fibrinogen interaction inhibitor with IC₅₀s of 5.00 and 2.72 μM in fluorescence polarization (FP) and AlphaLISA assays, respectively. RU-505 is highly permeable to the BBB. RU-505 reduces cerebral amyloid angiopathy (CAA). RU-505 can be used for the research of Alzheimer’s disease (AD).

Silybin (Silibinin B) (Standard) is the analytical standard of Silybin B (HY-N7046). This product is intended for research and analytical applications. Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity.

FAM labled Lepodisiran (LY3819469) sodiumis a FAM labled Lepodisiran sodium. Lepodisiran sodium is a GalNAc-conjugated small interfering RNA lipid-lowering agent. Lepodisiran sodium targets the hepatic LPA gene and degrades apolipoprotein (a) mRNA to silence its expression, thereby effectively reducing the production of apolipoprotein (a) and serum lipoprotein (a) in a dose-dependent manner. Lepodisiran sodium can be used in studies related to atherosclerotic cardiovascular disease.