Amyloid-β Inhibitor

TBPB (tert-butyl peroxybenzoate) is a highly selective, blood-brain-permeable M1 mAChR allosteric agonist (EC₅₀=289 nM) with anti-schizophrenia and anti-inflammatory activities. TBPB can enhance the sensitivity of M1 receptors to acetylcholine, activate downstream signaling pathways, and inhibit the release of pro-inflammatory cytokines (TNF-α, IL-6). TBPB can regulate the processing of amyloid and can be used in the study of neurodegenerative diseases (such as Alzheimer's disease) and inflammation-related diseases (such as sepsis).

gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. gamma-secretase modulator 6 inhibits Aβ42 secretion in HEK cell line stably expressing APP (Aβ amyloid precursor protein) (pIC₅₀: 8.1). gamma-secretase modulator 6 can be used for research of Alzheimer's disease.

Glimepiride (Standard) is the analytical standard of Glimepiride. This product is intended for research and analytical applications. Glimepiride (Glimperide) is a medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.

Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.

Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).

Sabirnetug is a humanized IgG2κ antibody targeting the Amyloid-β A4 precursor protein.

Prostaglandin A1 is a dehydrated derivative of Prostaglandin E1. Prostaglandin A1 exhibits antiviral, anti-inflammatory, antitumor, neuroprotective, and antihypertensive activities. Prostaglandin A1 covalently binds to cysteine residues of target proteins through Michael addition, or activates pathways such as PPARγ and HSPs via transcriptional regulation. Prostaglandin A1 is used in research on Mayaro virus infection, stroke, Alzheimer's disease, neuroblastoma, melanoma, and severe gestational hypertension.

BACE1-IN-1 is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC₅₀ values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 reduces cerebral Aβ40 levels in mice. BACE1-IN-1 can be used in studies related to Alzheimer's disease and type 2 diabetes.

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.

Eprodisate (70% in water) is an amyloid inhibitor that interferes with the interaction between amyloidogenic proteins and glycosaminoglycans, thereby inhibiting the aggregation of amyloid fibrils and the deposition of fibrils in tissues. Eprodisate (70% in water) slows the progression of renal disease associated with AA amyloidosis and may be useful for other types of amyloidosis.

Y040-7904 is a mitophagy activator. Y040-7904 enhances mitophagy by promoting mitochondria transport to autophagosomes and the fusion of autophagosomes with autolysosomes. Y040-7904 induces mitophagy through the SIRT1/FoxO3 pathway. Y040-7904 upregulates the levels of Parkin, PINK1, and LC3II/I. Y040-7904 reduces amyloid-β (Aβ) accumulation in both in vitro and in vivo models of Alzheimer’s disease.

CS-6253 TFA is an agonist of ABCA1. CS-6253 TFA can regulate lipoprotein metabolism, promote high-density lipoprotein biogenesis, and cellular cholesterol efflux. CS-6253 TFA also has certain neuroprotective effects and can clear Aβ from the brain. CS-6253 TFA can be used for research on cholesterol metabolism and diseases such as Alzheimer’s disease.

Stictic acid is a Depsidone. Stictic acid is found in the edible lichens Lobaria pindarensis and Lobaria pulmonaria. Stictic acid inhibits LPS/Aβ₄₂-induced mRNA expression of iNOS, IL-1β, TNF-α, and IL-6, and decreases LPS-induced COX-2 protein expression. Stictic acid inhibits Aβ₄₂ fibril formation and aggregation. Stictic acid scavenges superoxide anions. Stictic acid exhibits anticancer activity against colon adenocarcinoma. Stictic acid is used in research on Alzheimer's disease and colon adenocarcinoma.

FRM-024 is a central nervous system-penetrant, orally active γ-secretase modulator and Aβ42 lowering agent. FRM-024 is used for the research of familial Alzheimer's disease.

Amyloid-β-IN-2 (Compound EX.112) is a selective γ-secretase inhibitor. Amyloid-β-IN-2 inhibits Aβ42 secretion in H4 cells with an EC₅₀ value of 226 nM. Amyloid-β-IN-2 is promising for research of Alzheimer's disease (AD) and other diseases related to Aβ deposition.

TFEB activator 3 (compound 45) exhibits TFEB activation and lysosome biogenesis capabilities. TFEB activator 3 has effect on TFEB nuclear translocation with 44% (10μM 3h) and 97 % (30 μM 3h). TFEB activator 3 plays an important role in Alzheimer’s disease (AD). TFEB activator 3 can pass blodd brain barrier.

Amyloid-β-IN-3 (EX.113) is a selective γ-secretase inhibitor. Amyloid-β-IN-3 inhibits Aβ42 secretion in H4 cells with an EC₅₀ value of 148 nM. Amyloid-β-IN-3 regulates the γ-secretase catalytic activity to decrease Aβ42 production, thereby alleviating neurotoxicity caused by Aβ deposition. Amyloid-β-IN-3 is promising for research of Alzheimer's disease (AD).

Xanthocillin X permethyl ether is a natural compound isolated from fungal extracts, with Aβ-42 lowering activity.

Bepridil (CERM 1978 (free base); Org 5730) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoK_ATP/sarcK_ATP channels. Bepridil acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.

CCKBR agonist-1 (Compound 3r1) is a Gq-protein-preferring cholecystokinin B receptor (CCKBR) agonist with an EC₅₀ of 35 pM. CCKBR agonist-1 significantly increases the survival rate of neurons, with an EC₅₀ of 37 pM. CCKBR agonist-1 can improve the cognitive decline in mice by upregulating α-secretase (ADAM10) and calcium signaling molecule PLCB4, reduce the number of amyloid β (Aβ) plaques, and promote long-term potentiation (LTP). CCKBR agonist-1 can be used for the study of Alzheimer's disease.