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microglial activation

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1410
    GsMTx4
    Maximum Cited Publications
    112 Publications Verification

    		 TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4
  • HY-B1829A
    Dexamethasone phosphate disodium
    10+ Cited Publications

    Dexamethasone 21-phosphate disodium

    		 Glucocorticoid Receptor TGF-β Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
    Dexamethasone phosphate disodium
  • HY-14536
    Methylene Blue
    25+ Cited Publications

    Basic Blue 9; CI-52015; Methylthioninium chloride

    		 Environmental Pollutants Monoamine Oxidase Guanylate Cyclase Microtubule/Tubulin NO Synthase Infection Neurological Disease Cancer
    Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene Blue is a photosensitizer and redox agent. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
    Methylene Blue
  • HY-Y0836
    Diethyl succinate
    3 Publications Verification

    Diethyl Butanedioate

    		 Environmental Pollutants Biochemical Assay Reagents Reactive Oxygen Species (ROS) Metabolic Disease Inflammation/Immunology
    Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings .
    Diethyl succinate
  • HY-P1410A
    GsMTx4 TFA
    Maximum Cited Publications
    112 Publications Verification

    		 TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4 TFA
  • HY-D0186
    2'-Deoxyuridine
    3 Publications Verification

    		 Endogenous Metabolite Thymidylate Synthase Infection
    2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
    2'-Deoxyuridine
  • HY-N6673
    Okanin
    2 Publications Verification

    		 Toll-like Receptor (TLR) NF-κB Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways .
    Okanin
  • HY-A0183
    Phosphatidylserine
    1 Publications Verification

    Phospholipids, phosphatidylserines; Serine glycerophosphatides

    		 Akt TGF-β Receptor Inflammation/Immunology
    Phosphatidylserine (Phospholipids) is a well-conserved anti-inflammatory and immunosuppressive signal. Phosphatidylserine is involved in membrane translocation and the activation of protein kinase C, participating in Akt signaling through its interaction with PIP3. The local exposure of Phosphatidylserine can interact with complement and other proteins, promoting microglial phagocytosis during critical periods of synaptic refinement. Phosphatidylserine can promote blood coagulation in the extracellular environment and acts as a "eat me" signal to clear out apoptotic cells. Phosphatidylserine can suppress inflammation in tissues by inducing TGF-β secretion and inhibiting immune responses .
    Phosphatidylserine
  • HY-175510
    TREM2 agonist-5

    		TREM receptor Neurological Disease
    TREM2 agonist-5 is the microglial lipid-sensing receptor (TREM2) agonist with a Kd of 71.36 μM. TREM2 agonist-5 is a racemic structural analog of the TREM2 agonist VG-3927 and exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells. TREM2 agonist-5 displays a superior in vitro pharmacokinetic profile to VG-3927. TREM2 agonist-5 can used for the study of Alzheimer’s disease .
    TREM2 agonist-5
  • HY-15322
    PRT062607
    4 Publications Verification

    P505-15; PRT-2607; BIIB-057

    		 Syk Apoptosis Caspase Inflammation/Immunology Cancer
    PRT062607 (P505-15; PRT-2607) is an orally active ATP-competitive Syk inhibitor with an IC50 value of 1 nM, and exhibits at least 80-fold selectivity over other kinases. PRT062607 blocks B cell antigen receptor-mediated activation, Fcε receptor 1-mediated basophil degranulation and microglial phagocytosis, and induces caspase-dependent apoptosis and microglial death. PRT062607 inhibits tumor growth and peripheral nerve injury-induced mechanical allodynia, and prevents neuronal loss. PRT062607 can be used in research related to rheumatoid arthritis, chronic lymphocytic leukemia, non-Hodgkin's lymphoma, neurodegenerative diseases and neuropathic pain .
    PRT062607
  • HY-148853
    SRI-42127
    1 Publications Verification

    		 HuR Others
    SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes .
    SRI-42127
  • HY-P99019
    Fremanezumab
    2 Publications Verification

    TEV-48125; LBR-101; PF-04427429; RN-307

    		 CGRP Receptor Neurological Disease Inflammation/Immunology
    Fremanezumab (TEV-48125) is a humanized lgG2 monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC50 values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC50 value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine .
    Fremanezumab
  • HY-D0958
    Methylene blue hydrate
    20+ Cited Publications

    Basic Blue 9 hydrate; CI-52015 hydrate; Methylthioninium chloride hydrate

    		 Guanylate Cyclase Monoamine Oxidase NO Synthase Microtubule/Tubulin Infection Inflammation/Immunology Cancer
    Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
    Methylene blue hydrate
  • HY-14536A
    Methylene blue (purity≥70%)

    Basic Blue 9 (purity≥70%); CI-52015 (purity≥70%); Methylthioninium chloride (purity≥70%)

    		 Environmental Pollutants Monoamine Oxidase Guanylate Cyclase Microtubule/Tubulin NO Synthase Infection Neurological Disease Cancer
    Methylene blue (purity≥70%) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue (purity≥70%) is a vasopressor and is often used as a dye in several medical procedures. Methylene blue (purity≥70%) through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue (purity≥70%) is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue (purity≥70%) is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
    Methylene blue (purity≥70%)
  • HY-153248
    PBR28

    		Biochemical Assay Reagents Neurological Disease Inflammation/Immunology
    PBR28 is a translocator protein (TSPO) binding positron emission tomography (PET) radiotracer with blood-brain barrier permeability . PBR28 binds to TSPO, a marker of microglial activation and neuroinflammation, and is used for neuroinflammation imaging in brain diseases and HIV-infected individuals .
    PBR28
  • HY-101364
    CHPG
    4 Publications Verification

    		 mGluR NF-κB ERK Akt Cardiovascular Disease Inflammation/Immunology
    CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways .
    CHPG
  • HY-N2259
    Curcumenol
    4 Publications Verification

    (+)-Curcumenol

    		 Cytochrome P450 Neurological Disease Inflammation/Immunology Cancer
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
    Curcumenol
  • HY-N0381
    Maackiain
    1 Publications Verification

    DL-​Maackiain

    		 Keap1-Nrf2 p38 MAPK NOD-like Receptor (NLR) NF-κB mTOR Monoamine Oxidase Nuclear Factor of activated T Cells (NFAT) PKC Apoptosis Pyroptosis Autophagy Dengue Virus Infection Neurological Disease Metabolic Disease
    Maackiain (DL-Maackiain) is an orally active multi-target inhibitor with anti-tumor activity and neuroprotective effects. Maackiain activates the AMPK, NLRP3 and Nrf2/HO-1 pathways, and inhibits key targets such as NF-κB, mTOR, MAO-B, NFATc1 and PKCδ, thereby precisely regulating processes including apoptosis, autophagy and pyroptosis. Maackiain also effectively inhibits microglial activation, osteoclast formation, and proliferation and invasion of tumor cells, and protects dopaminergic neurons from damage. Maackiain is applicable to the research of various diseases such as Alzheimer's disease, osteoporosis, sepsis and dengue fever 。
    Maackiain
  • HY-P6442
    Chemerin15

    		Chemerin Receptor Syk ERK Src p38 MAPK P-selectin Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Chemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury .
    Chemerin15
  • HY-B1239
    Drofenine hydrochloride
    1 Publications Verification

    Hexahydroadiphenine hydrochloride

    		 Cholinesterase (ChE) Potassium Channel Amyloid-β TRP Channel Tau Protein NOD-like Receptor (NLR) JNK NF-κB IKK Neurological Disease Metabolic Disease Inflammation/Immunology
    Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm .
    Drofenine hydrochloride
  • HY-129724A
    α-MSH (11-13) acetate

    ACTH-(11-13) acetate; Lys-Pro-Val acetate; H-Lys-Pro-Val-OH acetate

    		 Infection Metabolic Disease
    α-MSH (11-13) acetate is a melanocortin-1 receptor ligand and anti-inflammatory agent. α-MSH (11-13) acetate triggers acute intracellular calcium elevation under specific costimulation or pathway inhibition conditions. α-MSH (11-13) acetate inhibits TNF-α-induced NF-κB activation, GPx activity, HIV replication, as well as colony formation of S. aureus and C. albicans. α-MSH (11-13) acetate is applicable to the research of Staphylococcus aureus infection, Candida albicans infection, human immunodeficiency virus infection, traumatic brain injury, corneal epithelial wound and inflammatory bowel disease .
    α-MSH (11-13) acetate
  • HY-P0240
    Tuftsin
    4 Publications Verification

    		 Endogenous Metabolite Inflammation/Immunology
    Tuftsin is a tetrapeptide. Tuftsin is a macrophage/microglial activator.
    Tuftsin
  • HY-178324
    T2M-010

    		TREM receptor Syk Neurological Disease Inflammation/Immunology
    T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD) .
    T2M-010
  • HY-P10227
    Xelafaslatide

    ONL-1204

    		 Fatty Acid Synthase (FASN) Apoptosis Interleukin Related Toll-like Receptor (TLR) NOD-like Receptor (NLR) Caspase Neurological Disease
    Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma .
    Xelafaslatide
  • HY-101364A
    CHPG sodium salt
    4 Publications Verification

    		 mGluR NF-κB ERK Akt Neurological Disease Inflammation/Immunology
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways. .
    CHPG sodium salt
  • HY-126066
    (-)-Syringaresinol

    		Drug Isomer NO Synthase NF-κB TNF Receptor Interleukin Related IFNAR COX CD20 CDK Bcl-2 Family Apoptosis Akt p38 MAPK GSK-3 Neurological Disease Inflammation/Immunology Cancer
    (-)-Syringaresinol is an orally active isomer of syringaresinol (HY-N8307) found in Annona Montana. (-)-Syringaresinol exhibits antioxidant, anti-inflammatory, and anticancer activities. (-)-Syringaresinol can alleviate ulcerative colitis via the PI3K-Akt/MAPK/Wnt signaling pathway. (-)-Syringaresinol inhibits HL-60 cell proliferation by arresting the G1 phase and inducing apoptosis. (-)-Syringaresinol inhibits LPS (HY-D1056)-induced microglial activation by downregulating the NF-κB p65 signaling pathway and its interaction with ERβ, exerting anti-neuroinflammatory effects .
    (-)-Syringaresinol
  • HY-171705
    KMS99220

    		Keap1-Nrf2 AMPK JNK IKK p38 MAPK NO Synthase α-synuclein Interleukin Related Neurological Disease
    KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .
    KMS99220
  • HY-N8371
    Shizukaol B

    		NO Synthase COX Interleukin Related TNF Receptor Inflammation/Immunology
    Shizukaol B is a lindenane-type dimeric sesquiterpene, used to be isolated from the whole plant of Chloranthus henryi. Shizukaol B has anti-inflammatory effect against lipopolysaccharide (LPS)-induced activation of BV2 microglial cells. Shizukaol B inhibits iNOS and COX-2, and suppresses NO production, TNF-α, and IL-1β expression .
    Shizukaol B
  • HY-101318
    β-Funaltrexamine hydrochloride
    2 Publications Verification

    β-FNA hydrochloride

    		 Opioid Receptor p38 MAPK STAT NF-κB NO Synthase Toll-like Receptor (TLR) Cardiovascular Disease Neurological Disease
    β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases .
    β-Funaltrexamine hydrochloride
  • HY-400882
    Tosylate-DPA-714

    		Drug Derivative Drug Intermediate TSPO Neurological Disease Inflammation/Immunology
    Tosylate-DPA-714 is a GMP-grade precursor for the radiosynthesis of DPA-714 (HY-122607). It crosses the blood-brain barrier and exhibits steroidogenic activity. DPA-714 is a specific ligand for the 18 kDa translocator protein (TSPO) with a Ki of 7.0 nM. Tosylate-DPA-714 is safe and does not bind to central benzodiazepine receptors (benzodiazepine receptor). As a radiolabeling precursor, Tosylate-DPA-714 reacts with 18F via nucleophilic aliphatic substitution to form 18F-DPA-714, enabling specific targeted binding to TSPO. 18F-DPA-714 accurately reflects the level of neuroinflammation mediated by microglial activation, and is used for PET molecular imaging of neurological diseases such as Alzheimer's disease and multiple sclerosis .
    Tosylate-DPA-714
  • HY-101546A
    Cavidine

    (+)-Cavidine

    		 p38 MAPK ERK Interleukin Related Neurological Disease Inflammation/Immunology
    Cavidine ((+)-Cavidine) is an analgesic and anti-inflammatory agent. Cavidine can be isolated from Corydalis ternata f. yanhusuo (Y.H.Chou & Chun C.Hsu) Y.C.Zhu. Cavidine reduces the expression of inflammatory factors IL-1β, IL-6 and TNF-α, and inhibits calcium ion influx. Cavidine inhibits the phosphorylation of p38 and ERK1/2. Cavidine increases mechanical and thermal pain thresholds in chronic pain models. Cavidine can be used for the research of chronic pain .
    Cavidine
  • HY-147512
    CB1/2 agonist 1

    		Cannabinoid Receptor Inflammation/Immunology
    CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis .
    CB1/2 agonist 1
  • HY-W049881
    9-Methyl-β-carboline

    		Dopamine Receptor PI3K Monoamine Oxidase Neurological Disease
    9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies .
    9-Methyl-β-carboline
  • HY-N10782
    Balanophonin

    		Apoptosis COX TNF Receptor p38 MAPK Neurological Disease Inflammation/Immunology Cancer
    Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis .
    Balanophonin
  • HY-110099
    (±)-NBI-74330

    		CXCR Inflammation/Immunology
    (±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
    (±)-NBI-74330
  • HY-14536R
    Methylene Blue (Standard)

    Basic Blue 9 (Standard); CI-52015 (Standard); Methylthioninium chloride (Standard)

    		 Reference Standards Guanylate Cyclase Monoamine Oxidase NO Synthase Microtubule/Tubulin Infection Neurological Disease Cancer
    Methylene Blue (Standard) is the analytical standard of Methylene Blue. This product is intended for research and analytical applications. Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
    Methylene Blue (Standard)
  • HY-123789
    T5342126
    1 Publications Verification

    		 Toll-like Receptor (TLR) Inflammation/Immunology
    T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.
    T5342126
  • HY-B1829
    Dexamethasone phosphate
    10+ Cited Publications

    Dexamethasone 21-phosphate

    		 Glucocorticoid Receptor TGF-β Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    Dexamethasone phosphate (Dexamethasone 21-phosphate) is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate is prepared by introducing a phosphate ester group to the hydroxyl group at position 21 of the Dexamethasone molecule. Dexamethasone phosphate inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease) .
    Dexamethasone phosphate
  • HY-D0186R
    2'-Deoxyuridine (Standard)

    		Reference Standards Endogenous Metabolite Thymidylate Synthase Infection
    2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) . In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
    Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
    In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
    2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
    2'-Deoxyuridine (Standard)
  • HY-W841438
    Lithium orotate

    		Amyloid-β Tau Protein Neurological Disease
    Lithium orotate is an orally active lithium supplement with reduced binding that can bypass amyloid sequestration in AD mice models. Lithium orotate can prevent Aβ plaque deposition and phospho-tau accumulation and reverse AD pathology, neuroinflammatory changes and memory loss in AD mice models and ageing wild-type mice. Lithium orotate can be used for the research of alcoholism and Alzheimer’s disease .
    Lithium orotate
  • HY-N2259R
    Curcumenol (Standard)

    (+)-Curcumenol (Standard)

    		 Reference Standards Cytochrome P450 Neurological Disease Inflammation/Immunology Cancer
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells .
    Curcumenol (Standard)
  • HY-150038
    NOSH-aspirin

    NBS-1120

    		 NF-κB Apoptosis Neurological Disease Cancer
    NOSH-aspirin (NBS-1120) is an orally active hybrid molecule that releases nitric oxide and hydrogen sulfide. NOSH-aspirin inhibits pancreatic cancer cell proliferation and induces apoptosis. NOSH-aspirin inhibits cancer cell growth and suppresses NF-κB and FoxM1 in a mouse model of pancreatic cancer. NOSH-aspirin also alleviates motor deficits and dopaminergic neuron degeneration in a rat model of Parkinson's disease. NOSH-aspirin reduces neuroinflammation caused by microglial and astrocytic activation. NOSH-aspirin can be used in research on cancers such as pancreatic cancer and neurological diseases such as Parkinson's disease .
    NOSH-aspirin
  • HY-D0958R
    Methylene blue hydrate (Standard)

    Basic Blue 9 hydrate (Standard); CI-52015 hydrate (Standard); Methylthioninium chloride hydrate (Standard)

    		 Reference Standards Guanylate Cyclase Monoamine Oxidase NO Synthase Microtubule/Tubulin Infection Inflammation/Immunology Cancer
    Methylene blue (hydrate) (Standard) is the analytical standard of Methylene blue (hydrate). This product is intended for research and analytical applications. Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
    Methylene blue hydrate (Standard)
  • HY-W778990
    2-Deoxyuridine-1,2,3,4,5-13C5

    		Isotope-Labeled Compounds Thymidylate Synthase Endogenous Metabolite Infection
    2-Deoxyuridine-1,2,3,4,5- 13C5 is the 13C-labeled 2'-Deoxyuridine (HY-D0186). 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
    2-Deoxyuridine-1,2,3,4,5-13C5
  • HY-175275
    10-Butyl Ether Minocycline

    BEM

    		 MMP Lipoxygenase Reactive Oxygen Species (ROS) Neurological Disease Inflammation/Immunology Cancer
    10-Butyl Ether Minocycline (BEM), a Minocycline (HY-17412A) derivative, is an MMP-8 and MMP-9 inhibitor with IC50s of 69.4 µM and 47.0 µM, respectively. 10-Butyl Ether Minocycline suppresses LPS (HY-D1056)-induced microglial activation. 10-Butyl Ether Minocycline inhibits VEGF-induced endothelial cell migration and L-Glutamine (HY-N0390)-induced ROS levels. 10-Butyl Ether Minocycline significantly reduces alcohol consumption in the Chronic Intermittent Ethanol (CIE) mouse model of alcohol dependence. 10-Butyl Ether Minocycline can be used for the study of neuroimmune-inflammatory diseases and Alcohol use disorder (AUD) .
    10-Butyl Ether Minocycline
  • HY-P0240A
    Tuftsin diacetate

    		Endogenous Metabolite Inflammation/Immunology
    Tuftsin diacetate, a tetrapeptide, is a macrophage/microglial activator.
    Tuftsin diacetate
  • HY-P10350
    PapRIV

    		NF-κB Neurological Disease Inflammation/Immunology
    PapRIV is an agonist of BV-2 microglial cells, capable of activating microglial cells through an NF-κB-dependent pathway. PapRIV induces the expression of pro-inflammatory cytokines such as IL-6 and TNFα and increases the production of reactive oxygen species (ROS). PapRIV can cross the blood-brain barrier .
    PapRIV
  • HY-155182
    HDAC-IN-62

    		HDAC Autophagy Neurological Disease Inflammation/Immunology
    HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain .
    HDAC-IN-62
  • HY-146168
    Nrf2 activator-5

    		Keap1-Nrf2 Inflammation/Immunology
    Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities .
    Nrf2 activator-5
  • HY-N1713
    29-Nor-20-oxolupeol

    		Others Neurological Disease
    29-Nor-20-oxolupeol, extracted from Impatiens basamina, reduces NO levels in LPS-activated murine microglial cells with an IC50 of 44.21 µM .
    29-Nor-20-oxolupeol

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