encephalomyelitis

Luzindole (N-0774) is a selective melatonin receptor antagonist that inhibits experimental autoimmune encephalomyelitis and exhibits antidepressant-like activity. It preferentially targets MT2 (Mel1b) over MT1 (Mel1a), with Ki values of 10.2 nM for human MT2 and 158 nM for MT1.

ASP-4058 is a selective, safe, and orally active second-generation agonist of sphingosine phosphate receptors 1 and 5 (S1P1 and S1P5).ASP-4058 ameliorates experimental autoimmune encephalomyelitis in mice.

AMG-369 (AMG 247) is an S1P1 S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats. encephalomyelitis in rats.

Tolperisone hydrochloride (Muscalm), a centrally acting muscle relaxant, is used in the therapy of pathologically increased tone of the cross-striated muscle resulted by neurological diseases (damage of the encephalomyelitis, myelopathy, multiple sclerosis, pyramidal tract) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

3-Methoxycatechol is a lignin-derived renewable chemical that promotes carcinogenesis in the esophagus.1,2-Dihydroxy-3-methoxybenzen exhibits strong antiviral activity against encephalomyelitis virus (EMCV).

BN201 (OCS-05) is a drug with neuroprotective and myelin repair effects, which acts mainly by activating serum glucocorticoid kinase-2 (SGK2), which in turn activates the FOXO3 pathway to promote neuronal survival and myelin repair. It is mainly used for the treatment of inflammatory neurological diseases such as multiple sclerosis (MS) and experimental autoimmune encephalomyelitis (EAE).BN201 is able to regulate multiple kinases in the insulin growth factor 1 (IGF1) pathway and cross the blood-brain barrier.

CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase AKT mTOR pathway and delays sensitive cells in late mitosis.

HPN-01 (IKK inhibitor XII) is a selective IKK inhibitor that inhibits IKK-α, IKK-β, and IKK-ε. HPN-01 reduces the severity of the disease, attenuates the immune imbalance, and prolongs the lifespan of mice in a model of autoimmune encephalomyelitis, and can be used to study immune disorders.

PF-04957325 is a potent and selective inhibitor of PDE8.PF-04957325 has an IC50 of 0.7 nM for PDE8A and 0.3 nM for PDE8B.PF-04957325 can be used to study autoimmune encephalomyelitis.

Cenerimod (ACT-334441) is an orally active, selective, and potent sphingosine 1-phosphate receptor (S1P1) agonist (EC50: 1 nM).Cenerimod inhibits multiple S1P isoforms and can be used to study murine experimental autoimmune encephalomyelitis (EAE) and murine scleroderma.

24, 25-Dihydroxy VD2 (24,25-Dihydroxy vitamin D2) is a metabolite of vitamin D2, which is the isomer of vitamin D present in the body as 25-hydroxyvitamin D. PF-04957325 is used in the study of autoimmune encephalomyelitis.

Nrf2 activator-12 (compound 10v) effectively activates Nrf2 (EC50=83.5 nM) and exhibits favorable pharmacological properties. It reverses disease progression and alleviates demyelination in a mouse model of experimental autoimmune encephalomyelitis.

ADWX 1 TFA is a novel peptide that potently targets and inhibits the Kv1.3 channel, with an IC50 of 1.89 pM. It specifically suppresses the activity of the Kv1.3 channel, in addition to inhibiting initial calcium signaling and NF-κB activation. This compound has been shown to ameliorate symptoms in rats with experimental autoimmune encephalomyelitis (EAE). ADWX 1 TFA is utilized in research focused on T-cell-mediated autoimmune diseases.

BNN27 is an agonist of the TrkA receptor (TrkAreceptor) and the p75NTR receptor (p75NTR receptor), exhibiting neurotrophic and anti-apoptotic properties. It enhances levels of glutamate, GABA, and glutamine in the hippocampus and prefrontal cortex of rats, improving glutamate turnover. In a mouse model of amyotrophic lateral sclerosis (ALS), BNN27 demonstrates neuroprotective effects, shows anti-inflammatory properties in an experimental autoimmune encephalomyelitis (EAE) model, and exhibits retinal protection in a rat diabetes model. BNN27 also possesses blood-brain barrier permeability.

RORγt inhibitor 4 (Compound 9a) is an orally active RORγt inhibitor capable of penetrating the central nervous system. It has been shown to improve experimental autoimmune encephalomyelitis.

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL J mice.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE). 5J-4 reduces the production of IL-17 and decreases the expression of RORα and RORγt.

NIBR-0213 is a potent and selective competitive S1P1 antagonist with activity against experimental autoimmune encephalomyelitis. In the GTPγ35S assay, it has IC50 values ​​of 2.0 nM and 2.3 nM for human and rat S1P1, respectively.

Ex26 (S1P1-IN-Ex26) is a selective and potent sphingosine 1-phosphate receptor 1 (S1P1) antagonist that disrupts SR-B1-S1PR1 interactions and inhibits S1P-S1PR1 signaling. Ex26 is used in experimental autoimmune encephalomyelitis, atherosclerosis, and gastric cancer.

BMS-520 is a potent, selective S1P1 agonist that has shown impressive efficacy when administered orally in a rat model of arthritis and in a mouse model of experimental autoimmune encephalomyelitis (EAE) with multiple sclerosis.

Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of inflammatory cytokines and chemokine evolved during active EAE. Bacoside A also has vasorelaxation.