neuroinflammation

Amantadine hydrochloride (CI-719) is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A and Parkinson disease.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

Dihydrolipoic acid (USAF XR-12), a dithiol-containing carboxylic acid, acts as a general antioxidant that is highly reactive against a variety of reactive oxygen species, including peroxynitirite, hydroxyl radicals, hydrogen peroxide, and hypochlorite, at concentrations ranging from 0.01-0.5 mM.

Amantadine (1-Aminoadamantane) is an antiviral, is a weak antagonist of the NMDA-type glutamate receptor, increases dopamine release, and blocks dopamine reuptake.

Tau-aggregation and neuroinflammation-IN-1 is a potent inhibitor of tau protein aggregates, showing significant inhibitory activity against AcPHF6 and full-length tau protein aggregates. It has anti-inflammatory activity, reduces NO release, exhibits low cytotoxicity against LSP-stimulated BV2 cells, and reverses okadaic acid-induced memory impairment in rats.

Anti-neuroinflammation agent 2 (compound 4) exhibits both anti-neuroinflammatory and antibacterial properties, with an IC50 value of 3.06 µM for TNF-α, an IC50 value of 4.31 µM for IL-6, and an EC50 value range of 0.87 to 3.16 µM for Gram-positive bacteria.

Compound A.10.3 (Anti-neuroinflammation agent 3) exhibits inhibitory activity against various Ser Thr kinases or receptor non-receptor tyrosine kinases.

Anti-neuroinflammation Agent 1 effectively modulates BV2 microglia cell polarization, shifting from an M1 to an M2 phenotype [1].

Deferoxamine(Desferrioxamine B) is an iron chelator (binds Fe(III) and many other metal cations) that inhibits neuronopathy, may be used to modify the reduction of iron accumulation and deposition in tissues, and may improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation following traumatic brain injury.Desferrioxamin-B has antioxidant, antiproliferative, Deferoxamine has antioxidant, antiproliferative, and antitumor activities, and can induce HIF-1α production, apoptosis and autophagy in cancer cells.Desferrioxamin-B can be used in the treatment of acute iron toxicity and COVID-19 related diseases.

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3 cAMP PKA signaling pathway after subarachnoid hemorrhage in rats.

Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long-chain fatty acid that inhibits fatty acid transport into cells. It is a potent and irreversible inhibitor of the mitochondrial respiratory chain and binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].

Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

Astramembrangenin (Cycloastragenol (Astramembrangenin)) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may have a novel therapeutic role in depression

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation.

Phenoxybenzamine is an α-1 adrenergic receptor antagonist. Phenoxybenzamine may exert a neuroprotective effect by reducing neuroinflammation after traumatic brain injury.

DPA-714 is a high-affinity translocator protein (TSPO) ligand (Ki=7 nM) designed with a fluorine atom, allowing labeling with fluorine-18 for in vivo imaging via positron emission tomography. [18F]DPA-714 successfully enables specific imaging of inflammation in various neuroinflammation models and a brain tumor model.

PB200, an HDAC6 inhibitor, demonstrates significant antidepressant effects with an IC50 value of 1.97 nM. It operates by normalizing aberrant HDAC6 expression levels and alleviating neuroinflammation.

DSPE-PEG(2000)-azide is a PEGylated derivative based on 1,2-distearoyl-sn-glycero-3-phosphoethanolamine (1,2-DSPE). This compound is utilized for attaching vascular cell adhesion molecule-1 (VCAM-1) antibodies to vesicles that encapsulate fingolimod, aiming to target the delivery of fingolimod to inflammatory vessels in mouse models simulating post-ischemic neuroinflammation. Additionally, DSPE-PEG(2000)-azide is employed to link fibrinogen mimetic peptides (FMP) to the surface of synthetic platelets used in treating uncontrollable bleeding caused by liver damage in mouse models.

Simufilamum (also known as PTI-125) is an oral small-molecule compound candidate that targets altered conformations of filamin A. It binds and reverts the misfolded filamin A in the brains of Alzheimer's disease patients, thereby slowing the disease's pathological progression. Additionally, PTI-125 reduces tau protein hyperphosphorylation, decreases Aβ42 aggregation and deposition, neurofibrillary tangles, and neuroinflammation. The compound demonstrates concentration-dependent efficacy in vitro, starting at 1 picomolar (pM), in both control groups and post-mortem hippocampal slices from Alzheimer's disease (AD) patients. PTI-125 is the first therapeutic candidate to preferentially bind and reverse pathogenic protein conformations.

TLR4 NF-κB-IN-1 (Compound 7x) is an orally bioavailable inhibitor targeting the TLR4 NF-κB signaling pathway, with anti-inflammatory properties and the ability to cross the blood-brain barrier. It can alleviate LPS-induced acute neuroinflammation in mice and downregulate the protein expression of TLR4, P-NF-κB, and P-IκB-α.