Multiple Sclerosis

EED-IN-4 is an orally active, EZH2-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC₅₀=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis.

ERβ agonist-2 (Page 72) is a selective ERβ agonist with an EC₅₀ of 800 nM or lower. ERβ agonist-2 selectively inhibits T cell activation and/or proliferation, thereby reducing circulating T cell levels in subjects, without exerting significant effects on circulating neutrophil, monocyte or B cell levels. ERβ agonist-2 is applicable to studies of chronic heart failure after myocardial infarction, as well as graft-versus-host disease, multiple sclerosis and experimental autoimmune encephalomyelitis.

BX-513 is a highly potent and selective CCR1 antagonist. BX-513 effectively inhibits the binding of radiolabeled MIP-1α and RANTES to CCR1, with K_i values of 40 nM and 60 nM, respectively. BX-513 suppresses MIP-1α-induced extracellular acidification, MIP-1α- and RANTES-induced intracellular calcium mobilization, as well as MIP-1α- and RANTES-induced migration of peripheral blood mononuclear cells. BX-513 can be used for the research of rheumatoid arthritis and multiple sclerosis.

Vitedoamine A is a Phenylnaphthalene-type lignan alkaloid. Vitedoamine A can be isolated from Vitex negundo. Vitedoamine A inhibits the activity of IKKβ with an IC₅₀ value of 39 μM. Vitedoamine A could inhibit the transcriptional activity of NF-κB, and suppress the production of NO and reduce the expressions of inflammatory cytokines (IL-1β, IL-6, and TNF-α). Vitedoamine A inhibits the phosphorylation of IKKα/β and p65, and prevents the degradation of IκBα. Vitedoamine A possesses anti-rheumatoid arthritis capacity.

BI-9774 is a potent, selective, and orally active AMPK activator, with EC₅₀ values of 20.0 nM and 63.1 nM against human AMPK α1β1γ1 and AMPK α1β2γ1, respectively. BI-9774 binds to the allosteric drug and metabolite (ADaM) site and induces ACC Ser79 phosphorylation in HepG2 cells, with an EC₅₀ of 83.2 nM. BI-9774 can be used in studies related to AMPK signaling, multiple sclerosis, and non-alcoholic fatty liver disease.

TBC-4746 is a α4β1/α4β7 integrin antagonist. TBC-4746 can be used in the research of asthma and multiple sclerosis.

BMS-520 is a potent, orally active and selective sphingosine-1-phosphate 1 (S1P₁) agonist with an EC₅₀ of 0.47nM. BMS-520 shows ~3400-fold selectivity over S1P₃. BMS-520 demonstrates impressive efficacy in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis. BMS-520 can be used for arthritis and EAE research.

Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine 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.

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

NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a K_d of 0.10 μM against NR4A1, and EC₅₀ values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis.

2ccPA (2ccPA18:1) is a metabolically stabilized carba analog of cyclic phosphatidic acid (cPA). 2ccPA inhibits autotaxin (ATX)‑mediated lysophosphatidic acid (LPA) production, suppresses extracellular matrix biosynthesis and elevates intracellular cAMP in fibrogenic skin fibroblasts. 2ccPA protects oligodendrocytes from mitochondrial‑driven apoptosis, suppresses neuroinflammation and demyelination, modulates microglial polarization and promotes rapid‑platelet/fibrin‑dependent hemostasis and subsequent fibrinolytic transition following brain injury.

Dioxadrol is an uncompetitive NMDA receptor (PCP binding site) antagonist, with a K_i value of 10.9 nM in pigs. Dioxadrol binds to the phencyclidine (PCP) binding site within the cation channel associated with the NMDA receptor, thereby blocking cation influx. Dioxadrol possesses local anesthetic, spasmolytic and central nervous system activities, including phencyclidine-like dissociative anesthetic properties. Dioxadrol can be used in the research of Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-associated dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, ischemic stroke, central nervous system trauma, and epilepsy.

ROCK-IN-13 is a ROCK2 inhibitor with an IC₅₀ of 8 nM against human ROCK2. ROCK-IN-13 has the potential for use in the research of diseases such as multiple sclerosis, glaucoma, and cardiovascular diseases.

Tolebrutinib (SAR442168) (Standard) is the analytical standard of Tolebrutinib (HY-109192). This product is intended for research and analytical applications. 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).

GSK-2262167 sodium is a selective S1P1 receptor agonist. GSK-2262167 sodium is used for research on inflammatory and immune diseases.

3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease.

RXR agonist 3 (Compound 35) is a potent, partial RXR agonist (EC₅₀s: 3, 3, 8 nM for RXRα, RXRβ, RXRγ, respectively). RXR agonist 3 can be used in the research of Alzheimer's disease, multiple sclerosis, and lymphoma.

Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine 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.