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BBB permeability

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Inhibitors & Agonists


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Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-150545

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro.
  • HY-144660

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability.
  • HY-151261

    HDAC Inflammation/Immunology
    HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.
  • HY-117983

    Amyloid-β Neurological Disease
    RU-505 is an effective β-amyloid ()-fibrinogen interaction inhibitor with IC50s of 5.00 and 2.72 μM in fluorescence polarization (FP) and AlphaLISA assays, respectively. RU-505 is highly permeable to the BBB. RU-505 reduces cerebral amyloid angiopathy (CAA). RU-505 can be used for the research of Alzheimer’s disease (AD).
  • HY-18738
    Pyrrolidinedithiocarbamate ammonium

    Ammonium pyrrolidinedithiocarbamate; PDTC ammonium; APDC

    NF-κB Inflammation/Immunology
    Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.
  • HY-N6685

    Others Cardiovascular Disease
    3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a blood-brain barrier (BBB) permeable mycotoxin.
  • HY-146049
    Antitrypanosomal agent 4

    Parasite Infection
    Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively.
  • HY-18749

    Akt Cancer Inflammation/Immunology Neurological Disease
    SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.
  • HY-131340

    Phosphodiesterase (PDE) Inflammation/Immunology
    LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.
  • HY-118152

    5-HT Receptor Neurological Disease
    Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
  • HY-21994
    Org-12962 hydrochloride

    5-HT Receptor Neurological Disease
    Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.
  • HY-141660

    Others Neurological Disease
    BSc3094 is a Tau aggregation inhibitor. BSc3094 can be used for the research of Alzheimer's disease (AD).
  • HY-146588
    NMDA receptor antagonist 4

    Others Neurological Disease
    NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease.
  • HY-144765

    NF-κB Apoptosis Inflammation/Immunology Neurological Disease
    NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research.
  • HY-144828
    RIP1/RIP3/MLKL activator 1

    RIP kinase Mixed Lineage Kinase Necroptosis Cancer
    RIP1/RIP3/MLKL activator 1 (Compound 6i) is a potent anti-glioma agent. RIP1/RIP3/MLKL activator 1 induces necroptosis through RIP1/RIP3/MLKL pathway. RIP1/RIP3/MLKL activator 1 exerts acceptable BBB permeability.
  • HY-144446

    Cholinesterase (ChE) Neurological Disease
    BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD.
  • HY-A0168


    Adenosine Receptor Cardiovascular Disease
    Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of drugs to the human CNS.
  • HY-144272

    Cholinesterase (ChE) 5-HT Receptor Serotonin Transporter Neurological Disease
    AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC50 value 2.29 nM against AChE, EC50 58.6 nM against 5-HT1A and IC50 value against SERT. Orally active.
  • HY-139604

    Apoptosis Cancer
    PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability.
  • HY-145833

    Epoxide Hydrolase Cholinesterase (ChE) Cancer Neurological Disease
    sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively.
  • HY-145833A

    Epoxide Hydrolase Cholinesterase (ChE) Cancer Neurological Disease
    sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively.
  • HY-150563

    Monoamine Oxidase Amyloid-β Inflammation/Immunology Neurological Disease
    Neuroinflammatory-IN-2 is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of 1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease.
  • HY-A0168S


    Adenosine Receptor Cardiovascular Disease Cancer
    Regadenoson-d3 (CVT-3146-d3) is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents.
  • HY-144392

    Cholinesterase (ChE) Neurological Disease
    AChE/BuChE-IN-1 (Compound 1), a chrysin derivative, is a selective butyrylcholinesterase (BuChE) inhibitor with an IC50 of 0.48 μM. AChE/BuChE-IN-1 inhibits acetylcholinesterase (AChE) with an IC50 of 7.16 μM. AChE/BuChE-IN-1 shows strong scavenging ·OH activities with a IC50 of 0.1674 μM. AChE/BuChE-IN-1 inhibits reactive oxygen species (ROS), Aβ1-42 aggregation (self-, Cu2+-induced, AChE-induced). AChE/BuChE-IN-1 has high BBB permeability and bioavailability and low cell toxicity. AChE/BuChE-IN-1 has the potential for Alzheimer' disease (AD) research.