multiple sclerosis

BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors.

SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Silperisone HCl (RGH-5002) blocks sodium and calcium channels in cells, decreases excitability and contractility of muscle cells, reduces peripheral tone, and acts as a muscle relaxant and peripheral vasodilator. Silperisone HCl is used to treat recurrent painful myoclonus due to spinal cord injury, abnormal hypertonia due to cerebrovascular disease, dystonia symptoms, cone tension syndrome, multiple sclerosis myospasm and myelitis. silperisone is a sodium channel protein type 2 alpha channel blocker. silperisone is an organosilicon similar to tolperisone, an organosilicon compound with centrally acting muscle relaxant properties.

DZ2002, an orally active, reversible, and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), exhibits significant immunosuppressive activity. It effectively prevents experimental dermal fibrosis by reversing the profibrotic phenotype in multiple cell types, making it useful for studying autoimmune diseases like lupus syndrome and systemic sclerosis.

CYM5181 is related to the body's immune system and can be used to study multiple sclerosis, transplant rejection, and adult respiratory distress syndrome.

Firategrast (SB 683699) is an orally active and specific α4β1 α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

Dimethyl fumarate (DMF) is an Nrf2 activator with oral activity and blood-brain barrier permeability. Dimethyl fumarate has antimicrobial, anti-inflammatory, and immunomodulatory activities and has been used in the study of multiple sclerosis.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

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.

Teriflunomide (A 77-1726) is the principal active metabolite of leflunomide, an approved therapy for rheumatoid arthritis and multiple sclerosis.

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

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.

BIA 10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) that increases levels of the neurotransmitter anandamide in the central nervous system and in peripheral tissues (that is, the rest of the body other than the brain and spinal cord). BIA 10-2474(BIA10-2474) interacts with the human endocannabinoid system. BIA 10-2474(BIA10-2474) was in development for the treatment of a range of different medical conditions from anxiety to Parkinson's disease, also for the treatment of chronic pain of multiple sclerosis, Y, hypertension or the treatment of obesity.

Tertiapin (reduced) is a synthetic bee venom peptide characterized by disulfide bonds between Cys3-Cys14 and Cys5-Cys18. It acts as an inhibitor of inward-rectifying potassium channels (potassium Channel) and can also block the activity of calcium-activated large conductance potassium channels. Tertiapin (reduced) is utilized in research related to diseases such as rheumatoid arthritis and multiple sclerosis.

BRD5075 is an effective activator of GPR65, stimulating the production of cAMP in a GPR65-dependent manner. Additionally, it reduces the gene expression of IL-1, IL-2, TNF, and chemokines. BRD5075 holds potential for researching multiple sclerosis and inflammatory bowel disease (IBD).

PSB-22269 is identified as a GPR17 antagonist with a Ki value of 8.91 nM. It exhibits significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies indicate that the binding site of PSB-22269 includes positively charged arginine residues and a hydrophobic pocket. PSB-22269 promotes myelin regeneration strategies, offering potential for multiple sclerosis research.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

IFB-088 acetate, a benzyl guanidine derivative, is used to treat diseases and cancers associated with the PPP1R15A pathway and associated with protein misfolding stress, Examples include tau disease, synaptic riboprotein disease, polyglutamine and polyalanine diseases, leukodystrophy, cystic fibrosis, multiple sclerosis, lysosome storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardiovascular diseases, osteoporosis, neurological trauma, and more.

Dalazatide (ShK-186) is a specific inhibitor of the Kv1.3 potassium channel, used in research on autoimmune conditions such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease [1] [2] [3].

PAD-IN-2, a potent inhibitor of PAD4 with an IC50 value <1 μM, can be utilized to study autoimmune diseases and cancers, including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, cystic fibrosis, ulcerative colitis, asthma, multiple sclerosis, and psoriasis.

γ-Fibrinogen377-395 TFA is an inhibitory peptide derived from fibrinogen, which also functions as a fibrinogen epitope. It effectively blocks microglial activation and impedes fibrin-Mac-1 interactions in vitro. Additionally, it exhibits in vivo efficacy by suppressing experimental autoimmune encephalomyelitis (EAE) in mice. This compound has applications in researching multiple sclerosis (MS) and other neuroinflammatory diseases linked to blood-brain barrier disruption and microglial activation [1].

Glatiramer acetate (GA) is a synthetic amino acid copolymer that is approved for treatment of relapsing remitting multiple sclerosis (RRMS) and clinically isolated syndrome (CIS).

Atacicept (TACI-Ig) is a homodimeric fusion protein that inhibits B-cell stimulation by binding to B-lymphocyte stimulatory factors and proliferation-inducing ligands, and can be used in the study of systemic lupus erythematosus, lupus nephritis, rheumatoid arthritis, multiple sclerosis, and various B-cell malignancies.