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primary microglia

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13

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13769A
    TPT-260 Dihydrochloride
    2 Publications Verification

    NSC55712; TPU-260 Dihydrochloride

    Drug Derivative Amyloid-β Beta-secretase Cardiovascular Disease Neurological Disease Inflammation/Immunology
    TPT-260 Dihydrochloride (NSC55712), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 Dihydrochloride increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 Dihydrochloride inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 Dihydrochloride improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 Dihydrochloride exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 Dihydrochloride can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease .
    TPT-260 Dihydrochloride
  • HY-P991480

    Transmembrane Glycoprotein Tau Protein Amyloid-β Neurological Disease Cancer
    ONC-841 is a blood-brain barrier-permeable, humanized monoclonal antibody targeting SIGLEC10. As an immune checkpoint inhibitor, ONC-841 restores the functions of immune effector cells such as T cells and enhances anti-tumor immune responses by blocking inhibitory signals mediated by SIGLEC10. ONC-841 restores the phagocytic and migratory activities of microglia, and promotes the phagocytosis of Amyloid-β and Tau protein aggregates by microglia. ONC-841 is applicable to research related to solid tumors and Alzheimer's disease .
    ONC-841
  • HY-160229

    R-1075 sodium

    Toll-like Receptor (TLR) MyD88 Caspase Reactive Oxygen Species (ROS) Autophagy Pyroptosis HIV Infection Neurological Disease
    ssRNA40 sodium (R-1075 sodium) is a single-stranded RNA40 derived from HIV-1. ssRNA40 sodium activates the TLR7, TLR8, TLR2, RIG-I, MDA5, MyD88, Caspase-3, IRE1α, NLRP3 inflammasome and IRF7 signaling pathways. ssRNA40 sodium alters mRNA expression in neutrophils, induces pro-inflammatory cytokines, ROS, autophagy (autophagy), pyroptosis (pyroptosis), neuronal death, neurodegeneration, aggregate formation and NK cell activation. ssRNA40 sodium activates the expression of CD62L, CD11b, CD69, MX1, OAS1, ATG7, LC3B and XBP1 in immune cell and neuronal populations. ssRNA40 sodium causes cortical neuron loss and axonal damage in mice in a TLR7-dependent manner. ssRNA40 sodium can be used in research on HIV-1 infection, neurodegeneration, COVID-19 and HIV-associated neurological disorders .
    ssRNA40 sodium
  • HY-173591

    Formyl Peptide Receptor (FPR) Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology
    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 .
    T0080
  • HY-107581
    MK-1903
    1 Publications Verification

    GPR109A MMP Metabolic Disease Inflammation/Immunology
    MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases .
    MK-1903
  • HY-111351

    Mixed Lineage Kinase Neurological Disease
    MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1 .
    MLK-IN-1
  • HY-P10019

    NLY01

    GCGR Neurological Disease Inflammation/Immunology
    Pegsebrenatide (NLY01) is a blood-brain barrier-penetrant GLP-1R agonist. Pegsebrenatide alleviates retinal inflammation and neuronal death secondary to ocular hypertension . Pegsebrenatide significantly delays onset and reduces disease severity in experimental autoimmune encephalomyelitis . Pegsebrenatide inhibits the formation of A1 reactive astrocytes in nerve cells and reduces the loss of retinal ganglion cells and dopaminergic neurons. Pegsebrenatide exerts neuroprotective effects in a mouse model of Parkinson's disease by directly preventing microglia-mediated conversion of astrocytes to the A1 neurotoxic phenotype. Pegsebrenatide can be used for research on glaucoma, Parkinson's disease, and multiple sclerosis .
    Pegsebrenatide
  • HY-12688

    Mitochondrial Metabolism Reactive Oxygen Species (ROS) Amyloid-β Neurological Disease Inflammation/Immunology
    Succinyl phosphonate is a α-Ketoglutarate Dehydrogenase Complex (KGDHC) modulator with neuroprotective activity. Succinyl phosphonate protects this complex, reduces cellular succinyl-CoA concentration, downregulates protein succinylation levels, and inhibits the activity of the α-ketoglutarate dehydrogenase complex. Succinyl phosphonate corrects hypoxic or ethanol-induced behavioral impairments, modulates exploratory behavior and emotional stress responses, and improves hypoxia tolerance. Succinyl phosphonate reduces glutamate excitotoxicity, restores the activity of the α-ketoglutarate dehydrogenase complex, reverses the changes in glutamate dehydrogenase and glutamine synthetase activities induced by β-amyloid (Amyloid-β), modulates cognitive function, and prevents β-amyloid-induced neuronal damage. Succinyl phosphonate improves microglial senescence, alleviates neuroinflammation, reactive oxygen species (ROS) production, lipid peroxidation, and the expression of proinflammatory cytokines. Succinyl phosphonate can be used in the research of Alzheimer's disease, aging-related neuroinflammation, and Parkinson's disease .
    Succinyl phosphonate
  • HY-13769

    TPU260

    Drug Derivative Beta-secretase Amyloid-β Cardiovascular Disease Neurological Disease Inflammation/Immunology
    TPT-260 (TPU260), a thiophene thiourea derivative, is a retromer complex stabilizer against thermal denaturation (Kd = ~5 µM). TPT-260 increases the levels of retromer proteins, shifts amyloid-precursor protein (APP) away from the endosome, and decreases the pathogenic processing of APP. TPT-260 inhibits TLR4 upregulation, IKKβ phosphorylation, NF-κB p65 nuclear translocation, and NLRP3 inflammasome formation. TPT-260 improves retromer-mediated cargo trafficking, reduces brain infarct area, and decreases amyloid plaque deposition. TPT-260 exhibits minimal cytotoxicity to primary microglia at tested concentrations. TPT-260 can be used for the research of inflammatory bowel disease, ischemic stroke and Alzheimer's disease .
    TPT-260
  • HY-N0859B

    NO Synthase Neurological Disease
    Schisanchinin D is an NO release inhibitor found in the fruits of Schisandra chinensis. Schisanchinin D can inhibit the release of nitric oxide (NO) by lipopolysaccharide (LPS)-activated microglia in primary murine BV2 microglia cells. Schisanchinin D is promising for research of neurodegenerative diseases such as Alzheimer's disease (AD) .
    Schisanchinin D
  • HY-N17383

    Toll-like Receptor (TLR) NF-κB Collagen Interleukin Related Cadherin NOD-like Receptor (NLR) TGF-β Receptor FXR Apoptosis Metabolic Disease Inflammation/Immunology
    Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease .
    Ligusticum cycloprolactam
  • HY-183593

    Phosphatase Akt Interleukin Related Neurological Disease
    SHIP1-IN-1 is an orally active, blood-brain barrier-permeable SHIP1 ligand. SHIP1-IN-1 exhibits IC50 values of 384 μM and 177 μM against human SHIP1, and an IC50 value of 379 μM against murine SHIP1. SHIP1-IN-1 alters the binding state of SHIP1 to phosphatidylinositol membranes, and regulates phosphoinositide pools and phosphorylated AKT levels. SHIP1-IN-1 enhances the uptake of myelin/membrane fragments and amyloid proteins by microglia, alters gene expression and reduces IL-1β levels. SHIP1-IN-1 can be used in studies related to Alzheimer's disease .
    SHIP1-IN-1
  • HY-182456

    KMO Neurological Disease
    CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease .
    CHDI-340246

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