Multiple Sclerosis

Rituximab is an anti-CD20 chimeric monoclonal antibody used for research of certain autoimmune diseases and cancer.

Rituximab (anti-CD20) is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer.

Tolebrutinib (SAR442168) is an orally active, selective, and blood-brain barrier-penetrant BTK inhibitor with neuroactive properties. Tolebrutinib is being investigated for use in multiple sclerosis (MS), particularly secondary progressive multiple sclerosis (SPMS)..

Inebilizumab is an anti-CD19 monoclonal antibody (mAb) with enhanced antibody-dependent cell-mediated cytotoxicity against B cells. Inebilizumab can be used for multiple sclerosis and neuromyelitis optica research.

MRT-6160 (Example 185) is an orally active VAV1 molecular glue degrader (DC₅₀: 7 nM). MRT-6160 reduces immune cell activation, immune cell proliferation and the production of various cytokines. MRT-6160 can be used for research of inflammatory or autoimmune disorder. MRT-6160 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc..

Nomelcitinib is a TYK2 inhibitor that modulates the IL23 signaling pathway. Nomelcitinib is used for research on multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease, systemic lupus erythematosus, psoriasis, psoriatic arthritis, Crohn's disease, Sjögren's syndrome, and scleroderma.

A-3190 is an orally active, blood-brain barrier permeable CD38 inhibitor, with an IC₅₀ of 7.25 nM against human CD38 and 1.24 nM against mouse CD38. A-3190 is a derivative of A-8531 (HY-184021), and it forms covalent adducts with NAD⁺ in the presence of CD38. A-3190 acts as an inducer of NAD⁺ levels and an inhibitor of NAM and ADPR levels. A-3190 increases NAD⁺ levels in the skin, lung, liver and brain of rodents, while reducing NAM and ADPR levels in brain tissues. A-3190 can be used in research related to multiple sclerosis, Parkinson's disease and Alzheimer's disease.

Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.

Atrosab is a humanized IgG1 antagonistic anti-TNFR1 antibody. Atrosab inhibits TNF-mediated Apoptosis induction and IL-6 and IL-8 production. Atrosab reduces neurological deficits. Atrosab can be used for research of inflammatory disease. The recommend isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).

Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4⁺ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses.

Natalizumab (Anti-CD49d) (AN100226; BG00002) Solution is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d), blocking the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab solution inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4⁺ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thereby exerting anti-inflammatory and immunomodulatory activity. Natalizumab (Anti-CD49d) solution is used in the study of relapsing-remitting multiple sclerosis (RRMS) and is also applied in the research of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab (Anti-CD49d) can also prevent lymphocytes from entering the central nervous system, thus preventing acute demyelinating relapses.

Flupirtine (D 9998) Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Inebilizumab (FUT8-KO) is an anti-CD19 monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the antibody-dependent cellular cytotoxicity (ADCC) effect of the antibody.Inebilizumab (FUT8-KO) exhibits enhanced ADCC against B cells and can be used for research on multiple sclerosis and neuromyelitis optica.

T0080 is a central nervous system-penetrant FPR1 inhibitor. By functionally blocking the FPR1 signaling pathway, T0080 effectively reduces neutrophil infiltration into ischemic brain tissue and maintains the integrity of the blood-brain barrier. T0080 alleviates tPA-associated hemorrhagic transformation, inhibits demyelination responses and the expression of NOX2. T0080 also possesses anti-apoptotic (apoptosis) and anti-inflammatory properties, thereby protecting myelin and reducing neurological deficits. T0080 is widely used in studies related to ischemic stroke complicated by hemorrhagic transformation after tPA thrombolysis, as well as multiple sclerosis.

PD 174265 is a highly selective, reversible EGFR/ErbB2 tyrosine kinase inhibitor (IC₅₀=0.45 nM) and cell differentiation inducer. By blocking receptor autophosphorylation and the downstream ERK signaling pathway (with an IC₅₀ of 0.45 μM for full-length ERK), PD 174265 effectively inhibits tumor growth and exhibits antitumor activity without obvious toxicity in in vivo models. PD 174265 drives oligodendrocyte precursor cells to switch from a proliferative state to a differentiated state, significantly upregulates the expression of myelin proteins such as CNP, PLP and MBP, and induces neurite branching. PD 174265 shows no inhibitory effect on other kinases including insulin, PDGF and basic FGF receptors, and serves as a crucial tool molecule for investigating the treatment of human epidermoid carcinoma and the mechanism of myelin repair in multiple sclerosis.

Opicinumab (BIIB033) is a human IgG1 monoclonal antibody targeting LINGO-1. Opicinumab binds LINGO-1 to block its negative regulatory signaling, suppress axonal degeneration, enhance axonal regeneration, promote remyelination, and exert neuroprotective effects. Opicinumab maintains axonal protective effects during co-administration with methylprednisolone. Opicinumab can be used for the research of multiple sclerosis, acute optic neuritis, and optic neuritis..

Flupirtine (D 9998) is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Nicotinic acid mononucleotide acts as a SARM1 inhibitor and a NAD⁺ biosynthesis intermediate, with an IC₅₀ value of 93.3 μM against SARM1. Nicotinic acid mononucleotide exerts axon-protective effects, delays axonal degeneration, elevates NAD⁺ levels, enhances Sirt1 activity, improves myocardial capillary density and alleviates myocardial fibrosis. Nicotinic acid mononucleotide reverses diabetic cardiomyopathy in diabetic mice by increasing myocardial NAD⁺ levels. Nicotinic acid mononucleotide is applicable to research related to cancer, multiple sclerosis, diabetic cardiomyopathy, neurodegenerative diseases and Huntington's disease.

PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC₅₀=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell. PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke.