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Pathways Recommended: Membrane Transporter/Ion Channel
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brain membranes

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63

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2

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3

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7

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7

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N2326

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM) .
    (±)-Anatoxin A fumarate
  • HY-18698

    iGluR Neurological Disease
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
    L-701324
  • HY-148246

    TGF-β Receptor Cancer
    MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability .
    MU1700
  • HY-P3883

    Neurokinin Receptor Neurological Disease
    [DAla4] Substance P (4-11) is an analog of Substance P (Substance P (HY-P0201)) that inhibits the binding of 125I-Bolton Hunter-conjugated Eledoisin (Eledoisin (HY-P0006)) (IC50 of 0.5 μM) and 125I-Bolton Hunter-conjugated Substance P (IC50 of 0.15 μM) to rat brain cortex membranes .
    [DAla4] Substance P (4-11)
  • HY-100821

    Bacterial Infection
    2,4-Dihydroxyphenylacetylasparagine is a potent and selective antagonist of glutamate. 2,4-Dihydroxyphenylacetylasparagine inhibits glutamate binding to rat brain synaptic membranes .
    2,4-Dihydroxyphenylacetylasparagine
  • HY-15084
    Dizocilpine maleate
    Maximum Cited Publications
    25 Publications Verification

    MK-801 maleate

    iGluR Neurological Disease
    Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
    Dizocilpine maleate
  • HY-110256
    N-Acetylcysteine amide
    5+ Cited Publications

    Reactive Oxygen Species Neurological Disease Inflammation/Immunology
    N-Acetylcysteine amide is a cell membranes and blood brain barrier permeant thiol antioxidant and neuroprotective agent, reduces ROS production.
    N-Acetylcysteine amide
  • HY-13510
    Cutamesine dihydrochloride
    2 Publications Verification

    SA4503 dihydrochloride; AGY94806 dihydrochloride

    Sigma Receptor Neurological Disease
    Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
    Cutamesine dihydrochloride
  • HY-119696S

    Isotope-Labeled Compounds Drug Metabolite Neurological Disease Cancer
    MTIC-d3 is deuterium labeled MTIC. MTIC is the active metabolite of Temozolomide (TMZ). MITC has lower bioavailability in the brain compared with TMZ, because the agent’s permeability through biological barriers and tumor cell membranes affects bioavailability. MITC exhibits low affinity to biological membrane[1].
    MTIC-d3
  • HY-12332
    JW 642
    2 Publications Verification

    MAGL Neurological Disease
    JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
    JW 642
  • HY-W017540
    Cyclocreatine
    1 Publications Verification

    Others Cardiovascular Disease
    Cyclocreatine is a Creatine analogue and acts as a potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine crosses membranes, enters the brain, and can be phosphorylated and dephosphorylated by creatine kinases .
    Cyclocreatine
  • HY-106745

    Ro 22-4839

    Calmodulin Cardiovascular Disease
    Elziverine (Ro 22-4839) is a brain circulation improvement agent with vasospasm antispasmodic effects. Elziverine is a calmodulin antagonist. Elziverine inhibits erythrocyte cell membrane rupture, platelet aggregation and lipid peroxidation .
    Elziverine
  • HY-14136
    Rimonabant
    5+ Cited Publications

    SR141716

    Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant
  • HY-160791

    Others Infection Cancer
    Claramine is a steroid polyamine with blood-brain barrier permeability. Claramine can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins .
    Claramine
  • HY-10712

    GlyT Neurological Disease
    Org-24598 is an inhibitor of glycine transporter 1 GlyT-1 . Org-24598 can inhibit the specific binding of [ 3H] CHIBIA-3007 to the rat brain membranes with a Ki value of 16.9 nM .
    Org-24598
  • HY-100937
    DPCPX
    5+ Cited Publications

    PD 116948

    Adenosine Receptor Cardiovascular Disease
    DPCPX (PD 116948), a xanthine derivative, is a highly potent and selective Adenosine A1 receptor antagonist, with a Ki of 0.46 nM in 3H-CHA binding to A1 receptors in rat whole brain membranes .
    DPCPX
  • HY-15249
    JZL 184
    2 Publications Verification

    MAGL Neurological Disease
    JZL 184 is a potent, selective and irreversible MAGL inhibitor that blocks 2-Arachidonoylglycerol (2-AG) hydrolysis in brain membranes (IC50 of 8 nM). JZL 184 displays >300-fold selectivity for MAGL over FAAH .
    JZL 184
  • HY-102064
    SR 57227A
    1 Publications Verification

    5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
    SR 57227A
  • HY-A0160

    LM 5008

    Serotonin Transporter Neurological Disease
    Indalpine (LM 5008) is a potent and selective 5-HT uptake blocker. Indalpine is potent in displacing 3H-5-HT bound to brain membranes with the IC50 of 36 μM . Indalpine, two antidepressant agent .
    Indalpine
  • HY-18236
    MDL-28170
    5+ Cited Publications

    Calpain Inhibitor III

    Proteasome Neurological Disease Inflammation/Immunology
    MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration . MDL-28170 also block γ-secretase .
    MDL-28170
  • HY-P10310

    HIV Infection
    F9170 is an amphipathic peptide with an activity of inactivate HIV-1 virions. F9170 targets the conserved cytoplasmic tail of HIV-1 env and disrupts the integrity of the viral membrane. F9170 is able to cross the blood-brain barrier (BBB) .
    F9170
  • HY-59201A

    nAChR 5-HT Receptor Neurological Disease
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
    A-582941 dihydrochloride
  • HY-15084B

    MK-801

    iGluR Neurological Disease
    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
    Dizocilpine
  • HY-118140

    Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
    ZCZ011
  • HY-14136S

    SR141716-d10

    Isotope-Labeled Compounds Cannabinoid Receptor Bacterial Infection Metabolic Disease Cancer
    Rimonabant-d10 is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
    Rimonabant-d10
  • HY-150407

    Ligands for Target Protein for PROTAC Autophagy Others Neurological Disease Cancer
    TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
    TSPO ligand-1
  • HY-10864
    URB-597
    4 Publications Verification

    KDS-4103

    FAAH Autophagy Mitophagy Neurological Disease
    URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity .
    URB-597
  • HY-U00322

    5-HT Receptor Neurological Disease
    5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM .
    5-HT3 antagonist 3
  • HY-119033

    MAGL Inflammation/Immunology
    MGL-IN-1 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. MGL-IN-1 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. MGL-IN-1 displays high membrane permeability and brain penetrant .
    MGL-IN-1
  • HY-108483

    Neurokinin Receptor Neurological Disease Inflammation/Immunology
    RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .
    RP 67580
  • HY-131688

    Others Inflammation/Immunology
    2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .
    2-Chlorohexadecanoic acid
  • HY-107855S

    (±)-Mevalonolactone-d7; Mevalolactone-d7

    Endogenous Metabolite Metabolic Disease
    DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
    DL-Mevalonolactone-d7
  • HY-111544

    Histone Methyltransferase Cancer
    EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .
    EML741
  • HY-P3138

    Angiotensin Receptor Cardiovascular Disease
    (Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. (Sar1)-Angiotensin II binds to brain membrane-rich particles, with a Kd of 2.7 nM. (Sar1)-Angiotensin II can stimulate protein synthesis and cell growth in embryonic chick myocytes .
    (Sar1)-Angiotensin II
  • HY-107855S1

    (±)-Mevalonolactone-d3; Mevalolactone-d3

    Endogenous Metabolite Metabolic Disease
    DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrial membrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
    DL-Mevalonolactone-d3
  • HY-160019

    Deubiquitinase Mitophagy Neurological Disease
    MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
    MTX115325
  • HY-W686216

    Ferroptosis Neurological Disease
    VK-28, a brain-permeable iron chelator, inhibits both basal and Fe/ascorbate-induced mitochondrial membrane lipid peroxidation, with an IC50 of 12.7 μM. VK-28 exhibits significant neuroprotective effects on ICV-6-OHDA. VK-28 can be used for the research of Parkinson’s disease and other neurodegenerative diseases .
    VK-28
  • HY-101654

    BN 50730; LAU-8080

    Platelet-activating Factor Receptor (PAFR) Cardiovascular Disease Inflammation/Immunology
    Rocepafant (BN 50730; LAU-8080) is a specific platelet activating factor (PAF) antagonist. Rocepafant can be used in rheumatoid arthritis and nervous system research .
    Rocepafant
  • HY-19578B

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity .
    Isamoltane hemifumarate
  • HY-120645

    Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
    BMS-986122
  • HY-E70007

    COMT

    Endogenous Metabolite Neurological Disease
    Catechol O-methyltransferase, porcine liver (COMT), the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain .
    Catechol O-methyltransferase, porcine liver
  • HY-10061

    AZD-3355

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
    Lesogaberan
  • HY-10061B

    AZD-3355 hydrochloride

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
    Lesogaberan hydrochloride
  • HY-144632

    Fungal Infection
    Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity .
    Antifungal agent 22
  • HY-B1102
    Evans Blue
    10+ Cited Publications

    Direct Blue 53; T-1824; C.I. 23860

    EAAT iGluR Neurological Disease
    Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
    Evans Blue
  • HY-W018643

    Methyl ferulate

    p38 MAPK Autophagy Neurological Disease Inflammation/Immunology Cancer
    Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties . Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders . Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages .
    Ferulic acid methyl ester
  • HY-P1318

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
    Ac-RYYRIK-NH2
  • HY-P1318A

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
    Ac-RYYRIK-NH2 TFA
  • HY-10061A

    AZD-3355 napadisylate

    GABA Receptor Metabolic Disease
    Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
    Lesogaberan napadisylate
  • HY-115340

    Biochemical Assay Reagents Others
    Decanoic acid sodium, also known as Decanoic acid sodium, is a salt of the fatty acid capric acid. It is easily soluble in water and has a slightly soapy smell. Decanoic acid sodium acts as a penetration enhancer, which means it increases the absorption and bioavailability of drugs across biological membranes, including the intestinal epithelium and the blood-brain barrier. This property makes it useful in pharmaceutical formulations to improve drug delivery and effectiveness. Furthermore, Decanoic acid sodium has potential applications in food preservatives and cosmetics due to its antibacterial properties.
    Decanoic acid sodium

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