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CNS

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280

Inhibitors & Agonists

5

Screening Libraries

1

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1

Biochemical Assay Reagents

28

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1

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2

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14

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156585

    Tau Protein Neurological Disease
    CNS-11 is a compoud that disaggregates tau fibrils. CNS-11 can be used for Alzheimer's disease (AD) research .
    <em>CNS</em>-11
  • HY-110097

    CNS 1102

    iGluR Neurological Disease
    Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
    Aptiganel hydrochloride
  • HY-101809A

    iGluR Cardiovascular Disease
    CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
    <em>CNS</em> 5161
  • HY-101809

    CNS 5161A

    iGluR Cardiovascular Disease
    CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
    <em>CNS</em>-5161 hydrochloride
  • HY-100356

    CNS 1102 free base

    iGluR Neurological Disease
    Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke .
    Aptiganel
  • HY-N5075

    Others Neurological Disease
    Quercetin 3-O-glucoside-7-O-rhamnoside is a member of flavonoid glycosides group with an inhibitory activity on the CNS .
    Quercetin 3-O-glucoside-7-O-rhamnoside
  • HY-162232

    mGluR Neurological Disease
    mGluR2 agonist 1 (Compound 5b) is a potent and selective metabotropic glutamate 2 receptor (mGluR) agonist with an EC50 of 82 nM. mGluR2 agonist 1 can be used for the research of central nervous system (CNS) diseases .
    mGluR2 agonist 1
  • HY-118098

    Beta-secretase Neurological Disease
    LY3202626 is a CNS penetrant BACE inhibitor with IC50s of 0.615 nM and 0.871 nM against BACE1 and BACE2, respectively .
    LY3202626
  • HY-144764

    5-HT Receptor Neurological Disease
    5-HT1A antagonist 1 (compound 6f) is a potent and selective antagonist of 5-HT1A receptor, with a Ki of 35 nM. 5-HT1A antagonist 1 can be used for the research of CNS diseases .
    5-HT1A antagonist 1
  • HY-132981

    P2X Receptor Neurological Disease
    Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases .
    Lu AF27139
  • HY-124382

    TRP Channel Neurological Disease
    AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research .
    AS1928370
  • HY-15722
    SB-222200
    2 Publications Verification

    Neurokinin Receptor Neurological Disease Endocrinology
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders .
    SB-222200
  • HY-107730

    Neuropeptide Y Receptor Neurological Disease
    NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor .
    NPY5RA-972
  • HY-122138

    mGluR Neurological Disease
    VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant .
    VU6010572
  • HY-110191

    mGluR Neurological Disease Cancer
    VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
    VU0469650
  • HY-B0250A

    BCH-189 salicylate

    HIV Reverse Transcriptase HBV Infection
    Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine salicylate
  • HY-133554

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM) .
    ASK1-IN-1
  • HY-147405

    PF-07284890; ARRY-461

    Raf Cancer
    Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAF V600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies .
    Tinlorafenib
  • HY-139279

    TPX-0131

    Anaplastic lymphoma kinase (ALK) Cancer
    Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
    Zotizalkib
  • HY-109189

    BPI-7711

    EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
    Rezivertinib
  • HY-P2457

    Bacterial Infection Inflammation/Immunology
    rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS .
    rCRAMP (rat)
  • HY-118158

    FAAH Neurological Disease
    FAAH/MAGL-IN-4 (Compound 13) is a potent fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitor with IC50s of 9.1 nM and 7.9 μM, respectively. FAAH/MAGL-IN-4 can be used for the research of pain and CNS disorders .
    FAAH/MAGL-IN-4
  • HY-10974
    MK-0752
    5+ Cited Publications

    γ-secretase Neurological Disease Cancer
    MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo .
    MK-0752
  • HY-144372

    TRP Channel Neurological Disease
    TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .
    TRPV1 antagonist 3
  • HY-144696

    DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-2
  • HY-154957

    mTOR Neurological Disease
    mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease .
    mTOR inhibitor-11
  • HY-147657

    GABA Receptor Neurological Disease
    GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
    GABAA receptor modulator-2
  • HY-131068

    Beta-secretase Neurological Disease
    BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay .
    BACE-1 inhibitor 2
  • HY-154958

    mTOR Neurological Disease
    mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases .
    mTOR inhibitor-12
  • HY-111263

    Amyloid-β Neurological Disease
    NIAD-4 is a fluorophore for optical imaging of amyloid-β () in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM .
    NIAD-4
  • HY-12776
    GSK805
    2 Publications Verification

    ROR Inflammation/Immunology
    GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .
    GSK805
  • HY-15043

    Bradykinin Receptor Inflammation/Immunology Endocrinology
    ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
    ELN-441958
  • HY-146068

    Others Neurological Disease
    AEP-IN-1 (Compound 13e) is a CNS agent-like non-covalent inhibitor of asparagine endopeptidase (AEP), with the IC50 of 89 nM. AEP-IN-1 can be used for the research of numerous neurological diseases such as Alzheimer’s disease (AD) .
    AEP-IN-1
  • HY-144695

    DYRK Neurological Disease
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
    Dyrk1A/α-synuclein-IN-1
  • HY-131181
    LEI-401
    1 Publications Verification

    Phospholipase Neurological Disease
    LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice .
    LEI-401
  • HY-W105505

    Biochemical Assay Reagents Neurological Disease Inflammation/Immunology
    SAMe-1,4-Butanedisulfonate, a natural compound, is a methyl donor in the central nervous system. SAMe-1,4-Butanedisulfonate has antidepressant activity. SAMe-1,4-Butanedisulfonate can be used for research of CNS disorders .
    SAMe-1,4-Butanedisulfonate
  • HY-145695

    Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-1 (compound 15) is an orally bioavailable CNS-permeant potent inhibitor of both human AChE (IC50=550 nM) and MAO B (IC50=8.2 nM). Dual AChE-MAO B-IN-1 behaves as a safe and metabolically stable neuroprotective agent, devoid of cytochrome liability .
    Dual AChE-MAO B-IN-1
  • HY-155079

    EGFR Cancer
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
    DZD1516
  • HY-124754

    BTRX-335140; CYM-53093

    Opioid Receptor Neurological Disease Metabolic Disease
    Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
    Navacaprant
  • HY-B0250
    Lamivudine
    5+ Cited Publications

    BCH-189

    HIV Reverse Transcriptase HBV Infection Cancer
    Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS .
    Lamivudine
  • HY-156438

    NOD-like Receptor (NLR) Neurological Disease
    NT-0796 is a selective and CNS-penetrant NLRP3 inflammasome inhibitor with an IC50 of 0.32 nM in PBMC assay. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 has the potential for neuroinflammatory diseases research .
    NT-0796
  • HY-119974

    NSC-253272

    DNA/RNA Synthesis Bacterial Infection Cancer
    Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide is a novel anticancer agent derived from a hydroxamic acid and has demonstrated to produce severe central nervous system (CNS) toxicity .
    Caracemide
  • HY-18679

    mGluR Neurological Disease
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
    TC-N 22A
  • HY-14905

    Tri-O-acetyl uridine

    Others Neurological Disease
    Uridine triacetate (Tri-O-acetyl uridine) is an orally active proagent of Uridine (HY-B1449). Uridine triacetate is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate is used for the research of 5-fluorouracil (5-FU) and capecitabine toxicity, or early-onset cardiac or central nervous system (CNS) .
    Uridine triacetate
  • HY-111232

    GHSR Metabolic Disease
    GSK894281 is an orally active and highly potent ghrelin receptor full agonist with a pEC50 of <4.9 at the human motilin receptor. GSK894281 effectively enters the CNS. GSK894281 has the potential for constipation or to assist in emptying the colon prior to colonoscopy or colon surgery research .
    GSK894281
  • HY-150503

    HDAC Neurological Disease
    KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
    KH-259
  • HY-N8441

    17β-Neriifolin

    Atg8/LC3 Na+/K+ ATPase Apoptosis Beclin1 Inflammation/Immunology Cancer
    Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells [2.
    Neriifolin
  • HY-122697

    Potassium Channel Cardiovascular Disease Neurological Disease Endocrinology
    ML418 is a potent, selective and CNS penetrating Kir7.1 potassium channel blocker. ML418 inhibits Kir7.1 with an IC50 value of 0.31 μM. ML418 can be used for the research of neurological, cardiovascular, endocrine and muscle disorders.
    ML418
  • HY-116016

    L-DOPA ethyl ester; Levodopa ethyl ester

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa
  • HY-116016A

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine .
    Etilevodopa hydrochloride

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