sclerosis

Oditrasertib (DNL-788) is a potent RIPKl inhibitor with an IC50 value of less than 100 nM.Oditrasertib can be used for the study of immune and neurological disorders such as multiple sclerosis and Alzheimer's disease.

Ozanimod hydrochloride (RPC-1063 hydrochloride) is an orally available, selective and potent sphingosine 1-phosphate (S1P) receptor modulator that shows high affinity for S1P1 and S1P5.Ozanimod has potential anticancer activity and can be used in the study of multiple sclerosis (MS), ulcerative multiple sclerosis (UMS), and other diseases. (MS), ulcerative colitis, coronavirus infections and myelodysplasia.

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.

14-Epiandrographolide is a compound derived from the above-ground parts of Andrographis paniculata that induces cell differentiation and can be used in the study of multiple sclerosis.

Aminaftone, a derivative of 4-aminobenzoic acid, inhibits endothelin-1 (ET-1) production and can be used to study hypertension and systemic sclerosis.

Myelin Basic Protein (87-99) Acetate (Myelin Basic Protein (87-99) Acetate (118506-26-6 Free base)) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein (87-99) Acetate causes a Th1 polarization in peripheral blood mononuclear cells, which is implicated in multiple sclerosis (MS).

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.

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

(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.

BJJF078, an aminopiperidine derivative, is a potent inhibitor of recombinant human and mouse glutamine aminotransferase (TG2) activity, with IC50 values of 41 and 54 nM for human and mouse glutamine aminotransferase, respectively.BJJF078 inhibits TG1 enzyme, with an IC50 of 0.16 μM.BJJF078 can be used to study multiple sclerosis (MS). BJJF078 can be used to study multiple sclerosis (MS).

Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP) and can be used in studies about the treatment of amyotrophic lateral sclerosis (ALS).

Utreloxastat (PTC857) is a novel 15-lipoxygenase inhibitor that can be used to study amyotrophic lateral sclerosis .

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.

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

Antroquinonol is a ubiquinone derivative from Antrodia camphorata with anti-inflammatory and anticancer activities.Antroquinonol reduces oxidative stress and inhibits inflammation and sclerosis in mice with focal segmental glomerulosclerosis through enhancement of the Nrf2 signaling pathway.Antroquinonol has potential for use in the treatment of non-small cell lung cancer. Antroquinonol has potential for the treatment of non-small cell lung cancer and may be used in colon cancer research.

Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

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

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

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.

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

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

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.

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].

Vatelizumab (GBR500), a monoclonal antibody, specifically targets the α2 subunit (CD49b) of very late antigen-2 (VLA-2) and is utilized in multiple sclerosis research [1].

CMB-087229 is an inhibitor of mutant superoxide dismutase 1 (SOD1) protein aggregation, exhibiting an IC50 of 67 nM, and holds potential for use in amyotrophic lateral sclerosis research [1].

Chrexanthomycin C, an orally active marine-derived natural product, exhibits significant bioactivities and shows a binding affinity for DNA [(G4C2)4 G4] with a dissociation constant (Kd) of 2.8 mM. This compound holds potential for neurodegenerative disease research, including amyotrophic lateral sclerosis (ALS) [1].

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

Di-Ellipticine-RIBOTAC is a bifunctional small molecule that effectively diminishes the r(G4C2) repeat expansion associated with c9ALS/FTD both in vitro and in vivo, showcasing therapeutic potential in amyotrophic lateral sclerosis (ALS) models.

Isoangustone A has antitumor activity, it can induce G1 cycle arrest in DU145 human prostate and 4T1 murine mammary cancer cells, it inhibits cell proliferation by targeting PI3K, MKK4, and MKK7 in human melanoma. Isoangustone A dampens mesangial sclerosis associated with inflammation in response to high glucose through hindering TGF-β and NF-κB signaling. Isoangustone A also shows strong ferric reducing activities and effectively scavenged DPPH, ABTS(+), and singlet oxygen radicals.

EPI-589, a quinone derivative and oxidoreductase enzyme inhibitor, is considered safe and well tolerated, showing promise for the treatment of amyotrophic lateral sclerosis (ALS).

Opicinumab (BIIB033) is a novel monoclonal antibody against LINGO-1 that may be used to prevent and delay acute optic neuritis and recurrent multiple sclerosis.

SOD1-Derlin-1 inhibitor 56-59 is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor 56-59 is potential in Amyotrophic lateral sclerosis (ALS) research.

Proteasome-activating peptide 1 enhances chymotrypsin-like proteasomal catalytic activity, boosting proteolytic rates both in vitro and within cultured cells. Additionally, it inhibits protein aggregation in a cellular model of amyotrophic lateral sclerosis [1].

Ozanezumab (GSK1223249) is a monoclonal antibody targeting Nogo-A (neurite outgrowth inhibitor A). It is utilized in research related to amyotrophic lateral sclerosis (ALS) and multiple sclerosis [1].

Myelin Basic Protein (MBP) fragment 146-170 is utilized in the study of Multiple Sclerosis (MS) [1].

Daclizumab (Zenapax) is a humanized monoclonal antibody that specifically inhibits the alpha subunit of IL-2R-HA. Daclizumab (Zenapax) can inhibit the binding of IL-2 and IL-2R-HA through specific binding to CD25. Daclizumab (Zenapax) studies multiple sclerosis.

γ-Fibrinogen377-395 is a peptide derived from fibrinogen, functioning both as an inhibitory molecule and an epitope. It inhibits microglial activation, disrupts fibrin-Mac-1 interactions in vitro, and mitigates experimental autoimmune encephalomyelitis (EAE) in murine models in vivo. This compound is relevant for research into multiple sclerosis (MS) and other neuroinflammatory disorders characterized by blood-brain barrier compromise and microglial activation [1].

Sampeginterferon beta-1a (BCD-054), a pegylated IFNβ-1a, is evaluated for its potential in research addressing remitting multiple sclerosis [1] [2].

Dihydroquinoline-pyrazoline DQP-997-74 (compound 2i) is a selective N-methyl-d-aspartate receptor (NMDAR) inhibitor that preferentially targets GluN2C/D subunits, with IC50 values of 0.069 μM and 0.035 μM, respectively, and possesses blood-brain barrier permeability. It enhances its inhibitory potency in a time-dependent manner when combined with the agonist glutamate, reducing epileptogenic events in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 is potentially applicable for the study of NMDAR-related neurological diseases [1].

Proteasome-activating peptide 1 TFA is a potent activator of the proteasome, enhancing chymotrypsin-like proteasomal catalytic activity and thereby increasing proteolytic rates both in vitro and in culture. Additionally, it inhibits protein aggregation in cellular models of amyotrophic lateral sclerosis (ALS) [1].

Dalazatide (ShK-186) TFA, a precise Kv1.3 potassium channel peptide inhibitor, is employed in researching autoimmune conditions, including multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease [1] [2] [3].

Tofersen (BIIB067) is an antisense oligonucleotide utilized to inhibit the synthesis of superoxide dismutase 1 (SOD1) protein by facilitating the degradation of SOD1 mRNA via the RNase H-dependent mechanism. This compound holds potential for amyotrophic lateral sclerosis (ALS) research.

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.

Briakinumab (ABT-874), a fully human anti-IL-12/23p40 monoclonal antibody, selectively targets and neutralizes IL-12 and IL-23. This compound is utilized in the research of various autoimmune disorders, including rheumatoid arthritis, inflammatory bowel disease, and multiple sclerosis [1].

PLP (180-199), an active biological peptide comprising amino acids 180-199 of myelin proteolipid protein (PLP)—the predominant myelin protein in the central nervous system (CNS)—is utilized in research focused on multiple sclerosis (MS), a chronic inflammatory demyelinating condition of the CNS.

Dirucotide (MBP8298), a synthetic 17-amino acid peptide, mirrors a segment of human myelin basic protein and has applications in research on central nervous system autoimmune disorders, including Multiple Sclerosis (MS) [1].

Alpha-Cobratoxin, a neurotoxin isolated from Thai cobra venom, displays neuromodulatory, antiviral, and analgesic activities, as well as potent immunosuppressive effects in the treatment of acute and chronic multiple sclerosis. It is currently under investigation for its potential application in adrenomyeloneuropathy [1].

Mirodenafil dihydrochloride is a PDE-5 inhibitor developed for the treatment of erectile dysfunction.

C18 3'-sulfo Galactosylceramide is a member of the sulfatide class of glycolipids. Levels of short-chain sulfatides, including C18 3'-sulfo galactosylceramide, decrease with age in mice and humans. It is increased in brain from mice with an arylsulfatase A deficiency (ASA-KO), particularly in lipid raft fractions. Plasma levels of C18 3'-sulfo galactosylceramide positively correlate with disability progression in patients with relapsing-remitting multiple sclerosis using the Expanded Disability Status Scale. It is also increased in plasma from patients with metachromatic leukodystrophy (MLD).

NF-κΒ Activator 2 is a potent, orally active compound that efficiently activates NF-κB with an EC50 value of 1.58 μM. By enhancing NF-κB expression and activation, it induces SOD 2 synthesis, rendering it useful for amyotrophic lateral sclerosis (ALS) research [1].