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Results for "

Astrocytes Inhibitors

" in MedChemExpress (MCE) Product Catalog:

40

Inhibitors & Agonists

1

Biochemical Assay Reagents

5

Peptides

6

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2

Isotope-Labeled Compounds

Targets Recommended:
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-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-101374A
    AGN 192403 hydrochloride

    (+)-BRD4780

    		 Imidazoline Receptor Caspase Mitochondrial Metabolism Lactate Dehydrogenase Cardiovascular Disease Neurological Disease Cancer
    AGN 192403 (BRD4780) hydrochloride is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 hydrochloride is also a TMED9 inhibitor. AGN 192403 hydrochloride shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 hydrochloride mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 hydrochloride can be used for glioma tumor and neurological diseases research .
    AGN 192403 hydrochloride
  • HY-15515
    SEA0400
    15+ Cited Publications

    		 Na+/Ca2+ Exchanger Cardiovascular Disease
    SEA0400 is a novel and selective inhibitor of the Na +-Ca 2+ exchanger (NCX), inhibiting Na +-dependent Ca 2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
    SEA0400
  • HY-14993
    SCH79797
    5 Publications Verification

    		 Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797
  • HY-D0889
    Glycylglycine
    1 Publications Verification

    Gly-Gly; H-Gly-Gly-OH

    		 Endogenous Metabolite Metabolic Disease
    Glycylglycine is a non-selective glycylglycine dipeptidase substrate and iNOS inhibitor. Glycylglycine can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis) .
    Glycylglycine
  • HY-107661
    Arundic Acid
    2 Publications Verification

    ONO-2506; (R)-2-Propyloctanoic acid

    		 ERK Akt NF-κB EAAT Cardiovascular Disease Neurological Disease
    Arundic Acid is an orally effective astrocyte function modulator and neuroprotective agent. Arundic Acid increases the expression and function of the astrocytic glutamate transporter EAAT1 by activating the ERK, Akt and NF-κB pathways. Arundic Acid attenuates retinal ganglion cell death in a normal-tension glaucoma model. Arundic Acid exerts neuroprotective effects in a mouse model of Parkinson's disease. Arundic Acid is a S100β protein synthesis inhibitor that prevents neurological deficits and brain tissue damage after intracerebral hemorrhage in rats. Arundic Acid downregulates neuroinflammation and astrocytic dysfunction after status epilepticus in immature rats. Arundic Acid is applicable to research related to Parkinson's disease, cerebral ischemia, glaucoma, intracerebral hemorrhage and epilepsy .
    Arundic Acid
  • HY-N0493
    Pectolinarigenin
    2 Publications Verification

    		 COX Lipoxygenase NF-κB p38 MAPK ERK HIF/HIF Prolyl-Hydroxylase Keap1-Nrf2 PI3K Apoptosis Autophagy Neurological Disease Inflammation/Immunology Cancer
    Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
    Pectolinarigenin
  • HY-160955
    Z218484536

    		Phosphatase Neurological Disease
    Z218484536 is a selective and brain-penetrant phosphoserine phosphatase (PSPH) inhibitor. Z218484536 binds to PSPH with a Kd value of approximately 0.23 μM. Z218484536 reduces L-serine and D-serine levels in astrocytes. Z218484536 is able to suppress spontaneous epileptic seizures without causing serious side effects. Z218484536 also shows good anti-epileptic effects in the temporal lobe epilepsy (TLE) model .
    Z218484536
  • HY-14994
    SCH79797 dihydrochloride
    5 Publications Verification

    		 Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797 dihydrochloride
  • HY-121362
    Evernic Acid

    		Bacterial Endogenous Metabolite TrxR Infection Neurological Disease Inflammation/Immunology Cancer
    Evernic Acid is an orally active thioredoxin reductase 1 (TrxR1) inhibitor and antiproliferative agent. Evernic Acid inhibits the proliferation and migration of human breast cancer cells. Evernic Acid blocks the NF-κB pathway by inhibiting p65 nuclear translocation and IκBα phosphorylation, thereby suppressing downstream inflammatory mediators. Evernic Acid acts as an antioxidant, anti-inflammatory agent and neuroprotective agent, protects neurons from cell death, mitochondrial dysfunction and oxidative stress damage, reduces astrocyte activation, and ameliorates dopaminergic neuron loss and neuroinflammation. Evernic Acid inhibits enoyl reductases FabI and FabZ of Plasmodium falciparum. Evernic Acid downregulates the expression of lasB and rhlA genes in Pseudomonas aeruginosa, inhibits quorum sensing and biofilm formation, and exerts antibacterial activity against Gram-positive bacteria, Gram-negative bacteria and fungi. Evernic Acid is applicable to research related to breast cancer, Parkinson's disease, bacterial infections and fungal infections .
    Evernic Acid
  • HY-B0327
    Irsogladine
    3 Publications Verification

    Dicloguamine

    		 Phosphodiesterase (PDE) NF-κB AP-1 TRP Channel Interleukin Related Inflammation/Immunology Cancer
    Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice . Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer [5][6] .
    Irsogladine
  • HY-113468A
    3-O-Methyldopa
    1 Publications Verification

    3-Methoxy-L-tyrosine; 3-O-Methyl-L-DOPA

    		 Drug Derivative Interleukin Related Neurological Disease Inflammation/Immunology
    3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa has certain antidepressant and neuroprotective activities. 3-O-Methyldopa can be used in the research of nervous system diseases such as depression and Parkinson's disease .
    3-O-Methyldopa
  • HY-19820A
    NSC45586 sodium
    1 Publications Verification

    		 Akt Ser/Thr Protease Apoptosis MMP Cardiovascular Disease Neurological Disease Inflammation/Immunology
    NSC45586 sodium is an inhibitor of PHLPP. NSC45586 sodium targets the PP2C phosphatase domains of PHLPP1 and PHLPP2, blocks the phosphatase activity of PHLPP, increases the expression level of FOXO1 in the nucleus, and reduces the protein expression of PHLPP1. NSC45586 sodium activates the AKT survival signaling pathway, enhances IGF-1-induced AKT activation, and inhibits the phosphorylation of AKT/ERK under basal conditions. NSC45586 sodium reduces staurosporine-induced neuronal death, preserves notochord cell morphology and KRT19 expression, inhibits cell apoptosis (apoptosis), improves the viability and proliferation of nucleus pulposus cells, upregulates the expression of ACAN/SOX9, and downregulates the expression of MMP13. NSC45586 sodium binds tightly to bovine serum albumin (bovine serum albumin), and exerts a more significant effect on nucleus pulposus in male individuals. NSC45586 sodium can be used in studies related to global cerebral ischemia and intervertebral disc degeneration .
    NSC45586 sodium
  • HY-121035
    7BIO

    7-Bromoindirubin-3-Oxime

    		 CDK GSK-3 Neurological Disease
    7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice [1].
    7BIO
  • HY-113468AS
    3-O-Methyldopa-d3

    3-Methoxy-L-tyrosine-d3; 3-O-Methyl-L-DOPA-d3

    		 Isotope-Labeled Compounds Drug Metabolite Interleukin Related Neurological Disease Inflammation/Immunology
    3-O-Methyldopa-d3 (3-Methoxy-L-tyrosine-d3) is deuterium labeled 3-O-Methyldopa (HY-113468A). 3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa has certain antidepressant and neuroprotective activities. 3-O-Methyldopa can be used in the research of nervous system diseases such as depression and Parkinson's disease .
    3-O-Methyldopa-d3
  • HY-P10019
    Pegsebrenatide

    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-120920
    UNC9995

    		Dopamine Receptor Inflammation/Immunology
    UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
    UNC9995
  • HY-D0889R
    Glycylglycine (Standard)

    Gly-Gly (Standard); H-Gly-Gly-OH (Standard)

    		 Reference Standards Endogenous Metabolite Metabolic Disease
    Glycylglycine (Standard) is the analytical standard of Glycylglycine (HY-D0889). This product is intended for research and analytical applications. Glycylglycine is a non-selective glycylglycine dipeptidase substrate and iNOS inhibitor. Glycylglycine can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis) .
    Glycylglycine (Standard)
  • 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-15515R
    SEA0400 (Standard)

    		Na+/Ca2+ Exchanger Reference Standards Cardiovascular Disease
    SEA0400 (Standard) is the analytical standard of SEA0400. This product is intended for research and analytical applications. SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX), inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.
    SEA0400 (Standard)
  • HY-149234
    MAO-B-IN-18

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-18 is a potent and selective MAO B inhibitor with IC50s of 52 nM and 14 μM for hMAO B and hMAO A, respectively. MAO-B-IN-18 enables promising cytoprotective effects against hydrogen peroxide insults in neuroblastoma and astrocytes cultures .
    MAO-B-IN-18
  • HY-101374
    AGN 192403

    (+)-BRD4780 free base

    		 Imidazoline Receptor Mitochondrial Metabolism Caspase Lactate Dehydrogenase Cardiovascular Disease Neurological Disease Cancer
    AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research .
    AGN 192403
  • HY-151919
    FAAH-IN-7

    		FAAH Inflammation/Immunology
    FAAH-IN-7 is a reversible and potent FAAH inhibitor with an IC50 value of 8.29 nM. FAAH-IN-7 suppresses oxidative stress in 1321N1 astrocytes and exhibits notable neuroprotective effect in ex vivo neuroinflammation model .
    FAAH-IN-7
  • HY-179214
    DEL-C1

    		Glycosidase Amyloid-β NF-κB Interleukin Related Neurological Disease
    DEL-C1 is a CHI3L1 inhibitor. DEL-C1 can restore the ability to clear Amyloid-β and repair lysosomal function of astrocytes. DEL-C1 can inhibit NF-κB signaling and IL-6 secretion. DEL-C1 can be used for the researches of inflammation and neurological disease, such as Alzheimer's disease .
    DEL-C1
  • HY-14993R
    SCH79797 (Standard)

    		Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797 (Standard)
  • HY-118489
    L644711

    		iGluR Neurological Disease Inflammation/Immunology
    L644711 is an anion transport inhibitor that reduces cell swelling by inhibiting potassium-activated D-aspartate release in astrocytes. L644711 can be used in the study of brain injury and neuroprotection .
    L644711
  • HY-10282
    Daglutril

    		Endothelin Receptor Others
    Daglutril is a compound with the potential to regulate cytokine-induced endothelin-1 production in astrocytes. In studies, it has an inhibitory effect on the production of endothelin-1 induced by some cytokines and can be used as a tool to screen compounds that inhibit endothelin-1 production in astrocytes.
    Daglutril
  • HY-149300
    SB-1436

    		Cholinesterase (ChE) Neurological Disease
    SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research .
    SB-1436
  • HY-118207
    LU-32-176B

    		GABA Receptor Cancer
    LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively .
    LU-32-176B
  • HY-W040074
    Glycylglycine hydrochloride hydrate

    Diglycine hydrochloride hydrate; Gly-Gly (HCl H2O)

    		 Biochemical Assay Reagents Metabolic Disease
    Glycylglycine hydrochloride hydrate is a non-selective Glycylglycine hydrochloride hydrate dipeptidase substrate and iNOS inhibitor. Glycylglycine hydrochloride hydrate can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine hydrochloride hydrate promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine hydrochloride hydrate can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis) .
    Glycylglycine hydrochloride hydrate
  • HY-14994R
    SCH79797 dihydrochloride (Standard)

    		Protease Activated Receptor (PAR) Apoptosis Cardiovascular Disease
    SCH79797 (dihydrochloride) (Standard) is the analytical standard of SCH79797 (dihydrochloride). This product is intended for research and analytical applications. SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
    SCH79797 dihydrochloride (Standard)
  • HY-113468AS1
    3-O-Methyldopa-d3 hydrate

    3-Methoxy-L-tyrosine-d3 hydrate; 3-O-Methyl-L-DOPA-d3 hydrate

    		 Isotope-Labeled Compounds Drug Metabolite Interleukin Related Neurological Disease Inflammation/Immunology
    3-O-Methyldopa-d3 (hydrate) is the deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa (3-Methoxy-L-tyrosine) hydrate is a metabolite of L-DOPA (HY-N0304) that can cross the blood-brain barrier (BBB). 3-O-Methyldopa hydrate inhibits the astrocyte-mediated protective effect of L-DOPA (HY-N0304) on dopaminergic neurons. In addition, 3-O-Methyldopa hydrate has certain antidepressant and neuroprotective activities. 3-O-Methyldopa hydrate can be used in the research of nervous system diseases such as depression and Parkinson's disease .
    3-O-Methyldopa-d3 hydrate
  • HY-172586
    GSK-3α/β-IN-1

    		GSK-3 PKA Neurological Disease Cancer
    GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM .
    GSK-3α/β-IN-1
  • HY-N0493R
    Pectolinarigenin (Standard)

    		Reference Standards COX Lipoxygenase NF-κB p38 MAPK ERK HIF/HIF Prolyl-Hydroxylase Keap1-Nrf2 PI3K Apoptosis Autophagy Inflammation/Immunology
    Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
    Pectolinarigenin (Standard)
  • HY-180899
    CHI3L1-IN-5

    		Glycosidase Amyloid-β NF-κB Neurological Disease
    CHI3L1-IN-5 (Compound Z17) is a highly selective CHI3L1 inhibitor with a KD value of 6 μM. CHI3L1-IN-5 restores the clearance ability of astrocytes by rejuvenating lysosomal function and Aβ uptake. CHI3L1-IN-5 alleviates neuroinflammation by inhibiting the NF-κB pathway. CHI3L1-IN-5 can be used for research on Alzheimer's disease .
    CHI3L1-IN-5
  • HY-182899
    DPAP

    		PERK Ras COX PD-1/PD-L1 Apoptosis DNA/RNA Synthesis Mitochondrial Metabolism Cancer
    DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma .
    DPAP
  • HY-180916
    CAII-IN-11

    		Carbonic Anhydrase Reactive Oxygen Species (ROS) NOD-like Receptor (NLR) Apoptosis Neurological Disease
    CAII-IN-11 (Compound A1) is a dual-target compound that contains a hCA II inhibitor (IC₅₀ = 2 nM) portion and a NO donor portion. CAII-IN-11 also has inhibitory activity against hCA IX, hCA XII, and hCA I, with IC50 values of 6, 3, and 152 nM respectively. CAII-IN-11 significantly increases the intracellular cGMP level in human trabecular meshwork cells. CAII-IN-11 reduces the apoptosis of retinal ganglion cells by reducing oxidative stress (ROS levels), inhibiting astrocytes and the NLRP3 inflammasome activation. CAII-IN-11 has hypotensive activity in rabbit models and can be used for the study of glaucoma .
    CAII-IN-11
  • HY-183352
    BuChE-IN-23

    		Cholinesterase (ChE) Toll-like Receptor (TLR) p38 MAPK Interleukin Related Complement System Neurological Disease
    BuChE-IN-23 is an orally active, blood-brain barrier permeable butyrylcholinesterase (eqBuChE) inhibitor with an IC50 of 15.59 μM and a Ki of 29.33 μM. BuChE-IN-23 exhibits an IC50 of 38.65 μM against hBuChE and shows selectivity for butyrylcholinesterase over acetylcholinesterase. BuChE-IN-23 inhibits LPS (HY-D1056)-induced nitric oxide production, attenuates hippocampal glial cell activation and neuroinflammation, suppresses the TLR4/p38 MAPK signaling pathway, and regulates the IL-1β/C3-mediated microglia-astrocyte inflammatory axis. BuChE-IN-23 can be used for the research of Alzheimer's disease .
    BuChE-IN-23
  • HY-155949
    Bt354

    		Neurological Disease Cancer
    Bt354 is an orally active STAT3 inhibitor with IC50 values of 4.6 μM (DU145), 6.5 μM (MDA-MB-435) and 7.2 μM (MDA-MB-231), respectively. Bt354 induces cell cycle arrest and apoptosis, and downregulates epithelial-mesenchymal transition-related genes. Bt354 exhibits anti-angiogenic and anti-inflammatory activities, attenuates the polarization of M1 microglia and A1 astrocytes, suppresses inflammasome-related signaling pathways, and alleviates mechanical hyperalgesia and thermal hyperalgesia. Bt354 can be used in research related to glioblastoma multiforme, triple-negative breast cancer, prostate cancer and neuropathic pain .
    Bt354

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