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permeability response

" in MedChemExpress (MCE) Product Catalog:

73

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1

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3

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1

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1

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1

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15

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7

Isotope-Labeled Compounds

1

GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16900
    Rolipram
    Maximum Cited Publications
    19 Publications Verification

    (R,S)-Rolipram; (±)-Rolipram; ZK 62711

    		 Bacterial HIV Phosphodiesterase (PDE) Epigenetic Reader Domain Amyloid-β Infection Neurological Disease Cancer
    Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis .
    Rolipram
  • HY-131370B
    Intralipid 20%
    4 Publications Verification

    		 Biochemical Assay Reagents Cancer
    Intralipid 20% is a safe fat emulsion that can be used as a nutritional supplement. Intralipid 20% effectively inhibits the opening of the mitochondrial permeability transition pore, effectively protecting the heart from ischaemia-reperfusion injury and has some potential to modulate the innate immune response .
    Intralipid 20%
  • HY-N0570
    Hydroxytyrosol
    Maximum Cited Publications
    7 Publications Verification

    DOPET; 3,4-Dihydroxyphenethyl alcohol; 3-Hydroxytyrosol

    		 Apoptosis Bacterial Reactive Oxygen Species (ROS) SARS-CoV Estrogen Receptor/ERR Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hydroxytyrosol (DOPET; 3,4-Dihydroxyphenethyl alcohol) is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields .
    Hydroxytyrosol
  • HY-B0464
    Hydralazine hydrochloride
    3 Publications Verification

    		 PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX Cardiovascular Disease Inflammation/Immunology Cancer
    Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
    Hydralazine hydrochloride
  • HY-109061
    Lazertinib
    3 Publications Verification

    YH25448; GNS-1480

    		 Apoptosis Akt TRP Channel EGFR ERK Infection Neurological Disease Metabolic Disease Cancer
    Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib
  • HY-125021
    2BAct
    3 Publications Verification

    		 Eukaryotic Initiation Factor (eIF) Neurological Disease
    2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
    2BAct
  • HY-110258
    ML334
    10+ Cited Publications

    LH601A

    		 Quinone Reductase Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    ML334
  • HY-N2468
    Xylobiose

    1,4-β-D-Xylobiose; 1,4-D-Xylobiose

    		 TNF Receptor Claudin HSP Metabolic Disease Inflammation/Immunology
    Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
    Xylobiose
  • HY-101379A
    8-Bromo-cGMP sodium
    5+ Cited Publications

    		 Calcium Channel Cardiovascular Disease Neurological Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K + . 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses .
    8-Bromo-cGMP sodium
  • HY-N16308
    ER-Laurdan

    		Fluorescent Dye Others
    ER-Laurdan is a derivative of the membrane-permeable fluorescent probe Laurdan (HY-D0080) that targets the endoplasmic reticulum (ER). As a membrane fluidity reporter, ER-Laurdan specifically localizes to the ER luminal membrane, and exhibits a prominent solvatochromic response to fluidity changes caused by membrane packing and exogenous saturated fatty acid stress. ER-Laurdan shows no overlapping localization with mitochondria, enables quantitative analysis of ER membrane fluidity via generalized polarization ratio measurement, and allows automatic signal masking with the help of ER markers. With high specificity and quantitative capability, ER-Laurdan serves as an important tool for investigating metabolic disorders and associated changes in the physical properties of cell membranes .
    ER-Laurdan
  • HY-N0745
    Senkyunolide I

    		Caspase ERK Keap1-Nrf2 Heme Oxygenase (HO) Apoptosis Neurological Disease Inflammation/Immunology
    Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A) . Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury .
    Senkyunolide I
  • HY-149555
    DNL343

    		Eukaryotic Initiation Factor (eIF) Neurological Disease
    DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
    DNL343
  • HY-149143
    JNJ-28583113
    5 Publications Verification

    		 TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-B1589A
    Carbinoxamine maleate salt
    1 Publications Verification

    		 Histamine Receptor Influenza Virus Infection Inflammation/Immunology
    Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
    Carbinoxamine maleate salt
  • HY-W016409
    Ethyl 3,4-dihydroxybenzoate
    1 Publications Verification

    Protocatechuic acid ethyl ester

    		 HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) NO Synthase Autophagy Apoptosis Metabolic Disease Cancer
    Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema .
    Ethyl 3,4-dihydroxybenzoate
  • HY-109061B
    Lazertinib mesylate
    3 Publications Verification

    YH25448 mesylate; GNS-1480 mesylate

    		 TRP Channel EGFR Akt ERK Apoptosis Cancer
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
    Lazertinib mesylate
  • HY-N0660
    Jujuboside B

    		Apoptosis PARP Caspase AMPK Autophagy VEGFR Keap1-Nrf2 STING 11β-HSD Ferroptosis PI3K Akt p38 MAPK ERK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
    Jujuboside B
  • HY-N0237
    Atractyloside A
    3 Publications Verification

    		 Toll-like Receptor (TLR) MyD88 NF-κB Mitochondrial Metabolism Interleukin Related Aquaporin Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Atractyloside A is an orally active inhibitor of the TLR4/MyD88/NF-κB signaling pathway and also an opener of the mitochondrial permeability transition pore (MPTP). Atractyloside A interferes with the activation of the TLR4/MyD88/NF-κB pathway, thereby inhibiting intestinal inflammatory responses. Atractyloside A reverses mucin synthesis impairment, improves intestinal barrier integrity, and restores homeostasis by altering the composition of the gut microbiota. Atractyloside A can be used in studies related to spleen deficiency diarrhea and myocardial injury .
    Atractyloside A
  • HY-121134
    Decylubiquinone
    1 Publications Verification

    		 Reactive Oxygen Species (ROS) Neurological Disease Cancer
    Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition .
    Decylubiquinone
  • HY-145607
    Zagociguat

    CY-6463; IW-6463

    		 Guanylate Cyclase Interleukin Related Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Zagociguat (CY-6463) is an orally active and BBB-permeable soluble guanylate cyclase (sGC) stimulator. Zagociguat can increase cGMP levels, regulate blood pressure, improve neuronal function, reduce inflammatory responses, and exert neuroprotective and cognitive-improving effects. Zagociguat can be used in the research of neurodegenerative diseases .
    Zagociguat
  • HY-131614
    TPC2-A1-N
    5+ Cited Publications

    		 Calcium Channel Others
    TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells .
    TPC2-A1-N
  • HY-114454
    INH14
    5 Publications Verification

    		 IKK Inflammation/Immunology Cancer
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity .
    INH14
  • HY-169841
    IHCH-7086

    		5-HT Receptor Arrestin Neurological Disease
    IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT2AR with a Ki of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression .
    IHCH-7086
  • HY-N6043
    Hydroxytyrosol acetate

    		Apoptosis Reactive Oxygen Species (ROS) Bacterial SARS-CoV Estrogen Receptor/ERR Infection Neurological Disease Inflammation/Immunology
    Hydroxytyrosol acetate is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol acetate not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol acetate effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol acetate significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol acetate has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields .
    Hydroxytyrosol acetate
  • HY-P991480
    ONC-841

    		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-12379
    NS-2028
    1 Publications Verification

    		 Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity . NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM . NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM . NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM) . NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability .
    NS-2028
  • HY-B0464A
    Hydralazine
    3 Publications Verification

    		 DNA Methyltransferase Reactive Oxygen Species (ROS) COX NO Synthase PGE synthase Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
    Hydralazine
  • HY-108391
    C8-Ceramide

    N-Octanoyl-D-erythro-sphingosine

    		 Apoptosis PKC Autophagy Inflammation/Immunology Cancer
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
    C8-Ceramide
  • HY-129079
    TFMB-(R)-2-HG
    3 Publications Verification

    		 Estrogen Receptor/ERR Histone Demethylase Fat Mass and Obesity-associated Protein (FTO) Cancer
    TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research .
    TFMB-(R)-2-HG
  • HY-164795
    SBI-810

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .
    SBI-810
  • HY-164795A
    SBI-810 hydrochloride

    		Neurotensin Receptor Arrestin iGluR ERK Sodium Channel Neurological Disease
    SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .
    SBI-810 hydrochloride
  • HY-12143
    Vofopitant dihydrochloride

    GR 205171A

    		 Neurokinin Receptor Neurological Disease
    Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
    Vofopitant dihydrochloride
  • HY-N0570R
    Hydroxytyrosol (Standard)

    DOPET (Standard); 3,4-Dihydroxyphenethyl alcohol (Standard); 3-Hydroxytyrosol (Standard)

    		 Reference Standards Apoptosis Bacterial Reactive Oxygen Species (ROS) SARS-CoV Estrogen Receptor/ERR Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hydroxytyrosol (Standard) (DOPET (Standard)) is the analytical standard of Hydroxytyrosol (HY-N0570). This product is intended for research and analytical applications. Hydroxytyrosol is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields .
    Hydroxytyrosol (Standard)
  • HY-112291
    SB 220025

    		p38 MAPK Src PKC Inflammation/Immunology
    SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
    SB 220025
  • HY-13976A
    PRL-8-53

    		Drug Derivative Neurological Disease
    PRL-8-53 is an orally active, blood-brain barrier-permeable benzoate derivative with potent spasmolytic activity and central nervous system regulatory activity. PRL-8-53 acts on dopamine, serotonin and cholinergic-related targets, enhances dopamine activity, partially inhibits serotonin function and elicits cholinergic responses, thereby maintaining neurotransmitter balance in the central nervous system. PRL-8-53 improves learning ability, short-term memory and long-term memory in animals. PRL-8-53 can be used in central nervous system-related research .
    PRL-8-53
  • HY-B0464S1
    Hydralazine-d5 hydrochloride

    		Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX Cancer
    Hydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
    Hydralazine-d5 hydrochloride
  • HY-W030338
    aPKC-IN-2

    		Endogenous Metabolite Inflammation/Immunology
    aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitory activity, providing the possibility for further development of small molecule aPKC inhibitors .
    aPKC-IN-2
  • HY-110258B
    (R,S,R)-ML334

    (R,S,R)-LH601A

    		 Drug Isomer Cancer
    (R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    (R,S,R)-ML334
  • HY-149431
    NDNA4

    		HSP Potassium Channel Cancer
    NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
    NDNA4
  • HY-12142
    Vofopitant

    GR 205171

    		 Neurokinin Receptor Neurological Disease
    Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .
    Vofopitant
  • HY-B0464S
    Hydralazine-d4 hydrochloride

    		Isotope-Labeled Compounds PGE synthase NO Synthase Reactive Oxygen Species (ROS) DNA Methyltransferase COX Cardiovascular Disease
    Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
    Hydralazine-d4 hydrochloride
  • HY-149823
    TRPV4 antagonist 4

    		TRP Channel Neurological Disease
    TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC50 value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury .
    TRPV4 antagonist 4
  • HY-N0570S
    Hydroxytyrosol-d4

    DOPET-d4; 3,4-Dihydroxyphenethyl alcohol-d4; 3-Hydroxytyrosol-d4

    		 Isotope-Labeled Compounds Apoptosis Bacterial Reactive Oxygen Species (ROS) SARS-CoV Estrogen Receptor/ERR Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hydroxytyrosol-d4 (DOPET-d4) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields .
    Hydroxytyrosol-d4
  • HY-N0570S1
    Hydroxytyrosol-d5

    DOPET-d5; 3,4-Dihydroxyphenethyl alcohol-d5; 3-Hydroxytyrosol-d5

    		 Isotope-Labeled Compounds Apoptosis Bacterial Reactive Oxygen Species (ROS) SARS-CoV Estrogen Receptor/ERR Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Hydroxytyrosol-d5 (DOPET-d5) is the deuterium labeled Hydroxytyrosol (HY-N0570). Hydroxytyrosol is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields .
    Hydroxytyrosol-d5
  • HY-119312
    C8 Dihydroceramide

    		PKC Cancer
    C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro .
    C8 Dihydroceramide
  • HY-N2468R
    Xylobiose (Standard)

    1,4-β-D-Xylobiose (Standard); 1,4-D-Xylobiose (Standard)

    		 Reference Standards TNF Receptor Claudin HSP Metabolic Disease Inflammation/Immunology
    Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is an orally active Claudin 2/CLDN2 inhibitor and HSP27 inducer. Xylobiose works by regulating intestinal barrier function and glucose and lipid metabolism-related signaling pathways. Xylobiose inhibits CLDN2 expression to reduce intestinal permeability, induces HSP27 to enhance cell protection, and regulates the miR-122a/miR-33a axis to inhibit liver lipid synthesis and improve insulin resistance. Xylobiose can strengthen intestinal barrier integrity, reduce blood sugar and blood lipid levels, and reduce oxidative stress and inflammatory response. Xylobiose can be used in the study of type 2 diabetes and metabolic syndrome .
    Xylobiose (Standard)
  • HY-16900R
    Rolipram (Standard)

    (R,S)-Rolipram (Standard); (±)-Rolipram (Standard); ZK 62711 (Standard)

    		 Reference Standards Bacterial HIV Phosphodiesterase (PDE) Epigenetic Reader Domain Amyloid-β Neurological Disease Cancer
    Rolipram (Standard) is the analytical standard of Rolipram (HY-16900). This product is intended for research and analytical applications. Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis .
    Rolipram (Standard)
  • HY-P10267
    Neuromedin (B-30)

    		Bombesin Receptor Neurological Disease Inflammation/Immunology
    Neuromedin B-30 is the neuropeptide, which is orignally isolated from porcine brain and spinal cord. , and may exhibit activity in stimulating smooth-muscle. Neuromedin B causes local vasodilation, increases vascular permeability and local hyperalgesia, thereby participating in neurogenic inflammation. Neuromedin B regulates appetite, body temperature, and behavioral responses to stress. Neuromedin B is also involved in regulating smooth muscle contraction and secretory function in the gastrointestinal tract .
    Neuromedin (B-30)
  • HY-W424851
    DPQ hydrochloride

    6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride

    		 PARP Infection Inflammation/Immunology
    DPQ hydrochloride is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ hydrochloride inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ hydrochloride can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
    DPQ hydrochloride
  • HY-B1589
    (±)-Carbinoxamine

    		Histamine Receptor Infection Inflammation/Immunology
    (±)-Carbinoxamine is a blood-brain barrier-permeable histamine H1 receptor antagonist. (±)-Carbinoxamine blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. (±)-Carbinoxamine inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. (±)-Carbinoxamine can be used in research on allergic rhinitis, influenza, etc.
    (±)-Carbinoxamine

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