Amyloid-β Inhibitor

Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.

MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.

Carnosine conjugated hyalyronate is a hyaluronic acid derivative functionalized with the dipeptide carnosine (Carnosine, Car) and has the ability to resist Aβ amyloid aggregation. Carnosine conjugated hyalyronate dissolves amyloid fibrils and reduces Aβ-induced toxicity in vitro. The effectiveness of Carnosine conjugated hyalyronate against amyloid aggregation is directly proportional to the Carnosine loading.

2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances.

CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC₅₀ of 0.3 μM. CGP52411 blocks the toxic influx of Ca²⁺ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.

Frentizole, an FDA-approved immunosuppressant, is a Aβ-ABAD (binding alcohol dehydrogenase) interaction inhibitor with an IC₅₀ value of 200 μM. Frentizole is used in studies of diseases related to rheumatoid arthritis and systemic lupus erythematosus.

10-Undecenoic acid zinc salt (Undecylenic acid zinc salt) is an antifungal agent. 10-Undecenoic acid zinc salt inhibits Aβ oligomerization, scavenges ROS and inhibits μ-calpain activity. 10-Undecenoic acid zinc salt has neuroprotective effects. 10-Undecenoic acid zinc salt has anticancer effects on a variety of tumors. 10-Undecenoic acid zinc salt inhibits C. albicans biofilm formation and MRSA infection. 10-Undecenoic acid zinc salt inhibits quorum sensing signals of Bacillus subtilis and Pseudomonas aeruginosa.

Phytic acid (myo-Inositol) potassium is an orally active compound. Phytic acid potassium can be derived from the seeds of legumes. Phytic acid potassium is a [PO4]³- storage depot and precursor for other inositol phosphates and pyrophosphates. Phytic acid potassium attenuates Aβ oligomers and upregulates autophagy protein. Phytic acid potassium can be used in cardiovascular disease, metabolic disease, nervous system disease and cancer research.

Azure C (Monomethylthionine) acts as a tau oligomer inhibitor and Aβ42 oligomerization inhibitor. Azure C regulates hsp70 ATPase activity, thereby mediating the clearance of tau protein. Azure C reduces the levels of toxic tau oligomers by promoting the formation of non-toxic tau aggregates, rescues neuroblastoma cells from tau oligomer-induced toxicity, and binds to and inhibits Aβ42 oligomerization. Azure C is generated via continuous oxidation of methylene blue or azure B through a horseradish peroxidase-mediated reaction. Azure C can be used in research related to tauopathies, including Alzheimer's disease.

Dehydroevodiamine hydrochloride is a blood-brain barrier-permeable, orally effective AChE and BACE1 inhibitor (IC₅₀ = 40.96 μM). Dehydroevodiamine hydrochloride is isolated and extracted from Evodia rutaecarpa. Dehydroevodiamine hydrochloride attenuates neurotoxicity through multiple targets by inhibiting BACE1 to block Aβ production, inhibiting AChE activity, scavenging ROS, and suppressing calcium influx. Dehydroevodiamine hydrochloride can be used for research on Alzheimer's disease, cerebral ischemia, vascular dementia, and other cognitive disorder-related diseases.

Semax acetate is a BBB-penetrable adrenocorticotropic hormone-like peptide and can form stable complexes with Cu²⁺. Semax acetate is a synthetic peptide analog of Adrenocorticotropic hormone (ACTH) (4-10). Semax acetate has immunomodulatory, nootropic and neuroprotective activities. Semax acetate can be used in the research of central nervous system diseases such as Alzheimer's disease and cerebral ischemia.

ELND 006 (Compound 30) is a metabolically stable γ-secretase inhibitor designed to selectively inhibit amyloid beta (Aβ) generation while sparing Notch signaling. It was developed through a synthetic strategy emphasizing diversity and chirality. ELND 006, along with its analog ELND007 (Compound 34), progressed into human clinical trials. In preclinical studies, both compounds demonstrated effective reduction of Aβ levels in vitro and in vivo. Comparisons with other γ-secretase inhibitors like Semagacestat, Begacestat, and Avagacestat underscored their potency and specificity in lowering Aβ levels in cerebrospinal fluid (CSF) of healthy human volunteers, suggesting potential therapeutic efficacy in Alzheimer's disease.

PF-719 is a highly selective Pyk2 inhibitor with an IC₅₀ value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases.

Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine (HY-N6608) and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.

Dihydrochalcone (3-Phenylpropiophenone) is a Aβ aggregation inhibitor. Dihydrochalcone destabilizes Aβ17-42 protofibrils by disrupting the β-sheet of β1 region. Dihydrochalcone destabilizes both U-shaped Aβ40/Aβ42 protofibrils and S-shaped Aβ42 protofibrils by binding to the protofibril cavity. Dihydrochalcone is the main component of daemonorops draco tree.

Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ₄₂-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam can be used for research of Alzheimer's disease.

Amilo-5MER (5-MP) TFA is an orally active and selective Serum Amyloid A (SAA) inhibitor. Amilo-5MER TFA specifically inhibits the release of pro-inflammatory cytokines IL-6 and IL-1β from SAA-activated cells. Amilo-5MER TFA reduces chronic inflammation and relieves symptoms of diseases such as rheumatoid arthritis (RA), inflammatory bowel disease (IBD), and multiple sclerosis (MS). Amilo-5MER TFA is promising for research of autoimmune diseases and chronic inflammatory diseases.

EP2 receptor antagonist-3 is a selective EP2 receptor antagonist (IC₅₀: 8 nM in hEP2 SPA assay, 50 nM in hEP2 cAMP assay). EP2 receptor antagonist-3 increases the macrophage-mediated clearance of Amyloid-β plaques. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases.

Zinc Phytate (myo-Inositol; hexakis dihydrogen phosphate; Inositol hexaphosphate) is an orally active compound. Zinc Phytate can be derived from the seeds of legumes. Zinc Phytate is a [PO4]³- storage depot and precursor for other inositol phosphates and pyrophosphates. Zinc Phytate attenuates Aβ oligomers and upregulates autophagy protein. Zinc Phytate can be used in cardiovascular disease, metabolic disease, nervous system disease and cancer research.

Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC₅₀ value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease.