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Alzheimer’s disease model

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

5

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-154851
    GSK-3 inhibitor 3

    		GSK-3 CDK Tau Protein Neurological Disease
    GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
    GSK-3 inhibitor 3
  • HY-123033A
    Nicotinamide riboside chloride
    Maximum Cited Publications
    14 Publications Verification

    		 Sirtuin Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
    Nicotinamide riboside chloride
  • HY-114331
    DLK-IN-1

    		MAP3K Neurological Disease
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
    DLK-IN-1
  • HY-153189
    TrkB-IN-1

    		Trk Receptor Neurological Disease
    TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research .
    TrkB-IN-1
  • HY-121191
    Bisnorcymserine

    N1,N8-Bisnorcymserine; (-)-Bisnorcymserine

    		 Cholinesterase (ChE) Neurological Disease
    Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
    Bisnorcymserine
  • HY-143464
    BChE-IN-4

    		Cholinesterase (ChE) Neurological Disease
    BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
    BChE-IN-4
  • HY-114234A
    TAK-070 Free base

    		Beta-secretase Neurological Disease
    TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model .
    TAK-070 Free base
  • HY-18112
    AZ-4217

    		Beta-secretase Neurological Disease
    AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research .
    AZ-4217
  • HY-161643
    S21-1011

    		Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
    S21-1011
  • HY-123033
    Nicotinamide riboside

    		Sirtuin Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
    Nicotinamide riboside
  • HY-123033B
    Nicotinamide riboside tartrate

    		Sirtuin Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Nicotinamide riboside tartrate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
    Nicotinamide riboside tartrate
  • HY-123033C
    Nicotinamide riboside malate

    		Sirtuin Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Nicotinamide riboside malate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
    Nicotinamide riboside malate
  • HY-123033D
    Nicotinamide riboside (triflate)

    		Endogenous Metabolite Sirtuin Neurological Disease Metabolic Disease Cancer
    Nicotinamide riboside (triflate), an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside (triflate) is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities . Nicotinamide riboside (triflate) reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease .
    Nicotinamide riboside (triflate)
  • HY-16969
    Dihexa
    5 Publications Verification

    PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2

    		 c-Met/HGFR Neurological Disease
    Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
    Dihexa
  • HY-117049
    Leucettine L41

    		CDK DYRK Neurological Disease
    Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
    Leucettine L41
  • HY-160939
    ASK1-IN-6

    		MAP3K Neurological Disease Inflammation/Immunology
    ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model .
    ASK1-IN-6
  • HY-156438
    NT-0796

    		NOD-like Receptor (NLR) Interleukin Related Neurological Disease
    NT-0796 is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. NT-0796 inhibits IL-1β release in human PBMC cells with an IC50 value of 0.32 nM. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. NT-0796 is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis .
    NT-0796
  • HY-W017540
    Cyclocreatine
    1 Publications Verification

    		 ATP Synthase Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
    Cyclocreatine
  • HY-126124
    AP39
    3 Publications Verification

    		 Others Cardiovascular Disease Neurological Disease
    AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research .
    AP39
  • HY-123976
    MPT0G211

    		HDAC Neurological Disease Cancer
    MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities .
    MPT0G211
  • HY-123976A
    MPT0G211 mesylate

    		HDAC Neurological Disease Cancer
    MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities .
    MPT0G211 mesylate
  • HY-151928
    JNK3 inhibitor-3

    		JNK Neurological Disease
    JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
    JNK3 inhibitor-3
  • HY-135115
    Oleuropein Aglycone

    3,4-DHPEA-EA

    		 Others Inflammation/Immunology
    Oleuropein aglycone is a polyphenol and an aglycone form of Oleuropein (HY-N0292) that has been found in extra virgin olive oil and has diverse biological activities. It is formed from oleuropein via enzymatic, acidic, or acetyl hydrolysis. Dietary administration of oleuropein aglycone (50 mg/kg of food) increases the number of neuronal autophagic vesicles and reverses cognitive deficits in a TgCRND8 transgenic mouse model of Alzheimer’s disease. It also decreases cortical and hippocampal levels of histone deacetylase 2 (HDAC2) and restores long-term potentiation in the same model. Oleuropein aglycone increases urinary norepinephrine, as well as interscapular brown adipose tissue epinephrine and UCP1 protein levels, and decreases plasma leptin levels and total abdominal cavity adipose tissue weight in a rat model of high-fat diet-induced obesity. It also reduces lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
    Oleuropein Aglycone
  • HY-W027553
    Ipidacrine

    NIK-247 free base

    		 Cholinesterase (ChE) Potassium Channel Sodium Channel Neurological Disease Metabolic Disease
    Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
    Ipidacrine
  • HY-158978
    Multitarget AD inhibitor-2

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Multitarget AD inhibitor-2 (Compound VN-19) is a multitargeting inhibitor acetylcholinesterase (AChE, IC50=0.14 μM), butyrylcholinesterase (BChE, IC50=11.6 μM), monoamine oxidase B (MAO B, IC50=0.45 μM). Multitarget AD inhibitor-2 inhibits self-induced aggregation of amyloid beta protein Aβ1-42 (inhibition rate is 47.3% at 20 μM), and downregulates the level of ROS in SH-SY5Y (80 inhibition rate at 25 μM). Multitarget AD inhibitor-2 ameliorates the cognitive decline in Scopolamine (HY-N0296)-induced Alzheimer’s Disease zebrafish models .
    Multitarget AD inhibitor-2
  • HY-124832
    δ-Secretase inhibitor 11
    1 Publications Verification

    		 Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
    δ-Secretase inhibitor 11
  • HY-D0186R
    2'-Deoxyuridine (Standard)

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

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