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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
83 Results for "
microglial activation
" in MedChemExpress (MCE) Product Catalog:
Products (83)
83 Results for "microglial activation" in MCE Product Catalog:
1
1 Cited Publications
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4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [ 3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP + or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease .
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1 Cited Publications
Cat. No.: HY-P1206
CAS No.: 174688-78-9
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CH 275 is a peptidic somatostatin analog that acts as an agonist of SST1 (IC50 = 30.9 nM, Ki = 52 nM). The IC50 values of CH 275 for sst3, sst4, sst2, and sst5 are 345 nM, >1 μM, >10 μM, and >10 μM, respectively. CH 275 binds to SSTR1 via the IAmp9-Asp137 ion pair interaction and the hydrophobic interaction between the isopropyl group of IAmp9 and Leu107, and reduces the extracellular acidification rate. CH 275 induces weak sst1 internalization, exerts immunosuppressive effects on macrophages, and decreases macrophage viability, MCP-1 expression/secretion, and IL-8 secretion, but does not alter proMMP-9 secretion or IL-8 mRNA levels. CH 275 reduces hippocampal β-amyloid levels and alleviates plaque pathology without inducing hippocampal microglial activation. CH 275 is used in research on Alzheimer's disease, Parkinson's disease, and depression .
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1 Cited Publications
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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.
Cat. No.: HY-175510
CAS No.: 3114105-24-4
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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 .
Synonyms: Basic Blue 9 (purity≥70%); CI-52015 (purity≥70%); Methylthioninium chloride (purity≥70%)
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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 .
Cat. No.: HY-P99185
CAS No.: 648895-38-9
Synonyms: AAB-001
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Bapineuzumab (AAB-001) is a humanized IgG1 monoclonal antibody that binds to the N-terminal region of amyloid beta in a helical conformation. Bapineuzumab induces microglial activation by upregulating CD11B, producing pro-inflammatory cytokines (IL-1β and TNFα), clearing plaques, and reducing insoluble and aggregated Aβ. Bapineuzumab can be used for research on Alzheimer's disease .
Cat. No.: HY-P6442
CAS No.: 1020407-90-2
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
Cat. No.: HY-178324
CAS No.: 364611-21-2
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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) .
Cat. No.: HY-P10227
CAS No.: 2040964-58-5
Synonyms: ONL-1204
Target:
Fatty Acid Synthase (FASN) Apoptosis Interleukin Related Toll-like Receptor (TLR) NOD-like Receptor (NLR) Caspase
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Cat. No.: HY-171705
CAS No.: 1478585-60-2
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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 .
Cat. No.: HY-N3201
CAS No.: 630057-39-5
Category:
Terpenoids Samanea saman (Jacq.) Merr. Other Diseases Diterpenoids Plants Disease Research Fields Labiatae Extract
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Cat. No.: HY-N8371
CAS No.: 142279-40-1
Cat. No.: HY-163565
CAS No.: 2770960-52-4
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BIIB129 is a covalent, selective, orally active, and brain-penetrant BTK inhibitor (Kd = 0.63 nM). BIIB129 binds to Cys481 and forms a hydrogen bond with Asn484, blocking BCR and FcγR signaling. BIIB129 inhibits B cell activation and proliferation, FcγR-induced microglial proliferation, FcγR-mediated ROS production in neutrophils, FcγR-induced TNF secretion in monocytes, and B cell-mediated antigen presentation to T cells. BIIB129 can be used for research on multiple sclerosis .
Cat. No.: HY-400882
CAS No.: 958233-17-5
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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 .
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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 .
Cat. No.: HY-W049881
CAS No.: 2521-07-5
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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 .
Cat. No.: HY-B1829AR
CAS No.: 2392-39-4
Synonyms: Dexamethasone 21-phosphate disodium (Standard)
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. 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).
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
