Amyloid-β Inhibitor

BSBM6 is a compound with the activity of inhibiting Aβ aggregation and regulating Aβ aggregation. BSBM6 can be demonstrated to inhibit Aβ aggregation through molecular dynamics simulation and related experiments, reducing soluble oligomers, and providing structural guidance for the design of new aggregation regulating ligands.

(±)Phenserine ((±)-Eseroline phenylcarbamate) is the racemic form of Phenserine (HY-103374). Phenserine is a derivative of Physostigmine (HY-N6608) and is an effective, non-competitive, long-acting and selective AChE inhibitor. Phenserine can reduce the formation of β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ). Phenserine can improve cognitive ability and slow down the progression of Alzheimer's disease.

Aβ-IN-8 (compound 7e) is a potent inhibitor of the Aβ aggregation.

MS1262 TFA is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC₅₀ of 19 nM and a K_d of 74 nM against G9a, and an IC₅₀ of 6 nM and a K_d of 19 nM against GLP. MS1262 TFA reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 TFA restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 TFA reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 TFA reduces the risk of thrombus rupture. MS1262 TFA can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer.

22(R)-Hydroxycholesterol-d₇ (Narthesterol-d₇) is the deuterated-labeled 22(R)-Hydroxycholesterol (HY-116969). 22 (R)-Hydroxycholesterol (Narthesterol) is a natural oxysterol, acting as a LXRα agonist that inhibits cancer cell proliferation. 22 (R)-Hydroxycholesterol activates LXRα-mediated upregulation of downstream ABCA1 expression, enhances apolipoprotein-dependent cholesterol efflux, reduces intracellular cholesterol content, and decreases the production of β-amyloid peptide. 22 (R)-Hydroxycholesterol induces the differentiation of human mesenchymal stem cells into functional dopaminergic neurons. 22 (R)-Hydroxycholesterol is applicable to research related to cancer, Alzheimer's disease, and Parkinson's disease.

BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC₅₀ value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease.

MAO-B-IN-48 is a selective MAO-B inhibitor (IC₅₀ = 0.09 μM, K_i = 0.02 μM). MAO-B-IN-48 exhibits inhibitory activity against hBChE (IC₅₀ = 1.10 μM, K_i = 0.43 μM) and AChE (IC₅₀ = 0.56 μM, K_i = 0.14 μM). MAO-B-IN-48 suppresses self-induced aggregation of toxic β-amyloid peptides and exerts antioxidant activity, including DPPH radical scavenging, CUPRAC copper ion reduction, and superoxide anion scavenging. MAO-B-IN-48 can be used for the study of Alzheimer's disease (AD).

PF-04382923 is a humanized IgG2Δa monoclonal antibody. PF-04382923 binds with high affinity to the free C-terminal regions of the amyloid-β peptides Aβ1-40 and Aβ1-42. PF-04382923 is indicated for the study of geographic atrophy (GA) associated with dry age-related macular degeneration (ARMD).

Glutaminyl cyclase/CB2R modulator-1 (Compound 18) acts as an inhibitor of glutaminyl cyclase (QC) (IC₅₀ = 0.65 μM) and an agonist of cannabinoid receptor type 2 (CB2R) (EC₅₀ = 0.32 μM). Glutaminyl cyclase/CB2R modulator-1 can be used for the research of Alzheimer's disease.

hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC₅₀s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ1_1-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.

Latrepirdine (dihydrochloride) (Standard) is the analytical standard of Latrepirdine (dihydrochloride). This product is intended for research and analytical applications. 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.

Rutin (hydrate) (Standard) is the analytical standard of Rutin (hydrate). This product is intended for research and analytical applications. Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress.

Thiethylperazine (dimaleate) (Standard) is the analytical standard of Thiethylperazine (dimaleate). This product is intended for research and analytical applications. Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.

Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.

CHF5022 is an inhibitor of Aβ42 secretion (IC₅₀=92 μM). CHF5022 retains a modest activity on Aβ40 at non-cytotoxic concentrations (−22.2±4.8% at 100 μM).

Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.

Valiltramiprosate-d₆ (ALZ-801-d₆) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.

Kayaflavone is an amentoflavone type biflavonoid. Kayaflavone has an inhibitory activity against amyloid-β42 cytotoxicity in PC-12 cells with an EC₅₀ value of 5.29 μΜ. Kayaflavone is promising for research of Alzheimer’s disease.

Azeliragon (Standard) is the analytical standard of Azeliragon. This product is intended for research and analytical applications. Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD). Azeliragon also can cross the blood-brain barrier (BBB).

Tolcapone 3-β-D-glucuronide (Ro 61-1448) is an O-methyl metabolite of Tolcapone (HY-17406) and is pharmacologically inactive. 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.