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central nervous system (CNS)

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13011
    Alectinib
    Maximum Cited Publications
    43 Publications Verification

    CH5424802; RO5424802; RG7853

    Anaplastic lymphoma kinase (ALK) Neurological Disease Cancer
    Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib
  • HY-13011A
    Alectinib Hydrochloride
    Maximum Cited Publications
    43 Publications Verification

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    Anaplastic lymphoma kinase (ALK) Neurological Disease Cancer
    Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib Hydrochloride
  • HY-14905

    Tri-O-acetyl uridine

    Drug Derivative 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-111263
    NIAD-4
    1 Publications Verification

    Fluorescent Dye Amyloid-β Others
    NIAD-4 is a blood-brain barrier permeable 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-B1330
    Proglumide
    1 Publications Verification

    Cholecystokinin Receptor Neurological Disease Endocrinology Cancer
    Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities .
    Proglumide
  • HY-105231
    Bryostatin 1
    2 Publications Verification

    PKC HIV Bacterial Infection Neurological Disease Inflammation/Immunology Cancer
    Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties .
    Bryostatin 1
  • HY-170554

    Antibody-Drug Conjugates (ADCs) Topoisomerase DNA/RNA Synthesis Inflammation/Immunology Cancer
    ABBV-706 is a SEZ6-targeted topoisomerase 1 inhibitor Antibody-Drug Conjugates (ADCs), which is composed of the Linker-Payload conjugation (HY-148820) and the Anti-SEZ6 Antibody (SC17) (HY-P991041). ABBV-706 can inhibit cancer cells proliferation and induce DNA damage and G2/M arrest. ABBV-706 exhibits high efficacy against small cell lung cancer (SCLC), neuroendocrine tumors (NENs) and central nervous system (CNS) tumors .
    ABBV-706
  • HY-P1333
    Dynorphin A
    1 Publications Verification

    Opioid Receptor Apoptosis Caspase Endogenous Metabolite Neurological Disease
    Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .
    Dynorphin A
  • HY-14951
    Firategrast
    5+ Cited Publications

    SB 683699

    Integrin Neurological Disease
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity .
    Firategrast
  • HY-15722
    SB-222200
    5+ Cited Publications

    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-B0770
    Artemotil
    1 Publications Verification

    β-Arteether; (+)-Arteether; Arteether

    CXCR Parasite Infection Cancer
    Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
    Artemotil
  • HY-149555

    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-172429

    ORIC-114

    EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
    Enozertinib
  • HY-10968
    CYM5442
    3 Publications Verification

    LPL Receptor Neurological Disease
    CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .
    CYM5442
  • HY-107790
    5-Methoxyflavone
    2 Publications Verification

    DNA/RNA Synthesis Neurological Disease
    5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
    5-Methoxyflavone
  • HY-109189
    Rezivertinib
    1 Publications Verification

    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-W019815

    ENU; N-Nitroso-N-ethylurea

    DNA/RNA Synthesis Neurological Disease Cancer
    N-Ethyl-N-nitrosourea (ENU) is a DNA alkylating agent. N-Ethyl-N-nitrosourea induces leukemia by alkylating nucleobases, disrupting DNA, and resulting in bone marrow suppression and the formation of leukemic cells. N-Ethyl-N-nitrosourea is teratogenic in vivo, inducing tumor formation and paw malformations in pregnant rats. N-Ethyl-N-nitrosourea cause central nervous system (CNS) tumors and genetic disorders .
    N-Ethyl-N-nitrosourea
  • HY-132806

    RG-7816; RO-7017773

    GABA Receptor Neurological Disease
    Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .
    Alogabat
  • HY-N2321
    Salsolinol-1-carboxylic acid
    1 Publications Verification

    Others Neurological Disease
    Salsolinol-1-carboxylic acid is an endogenous alkaloid in the central nervous system (CNS) .
    Salsolinol-1-carboxylic acid
  • 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-P3609
    CR 665
    2 Publications Verification

    JNJ 38488502; FE 200665

    Opioid Receptor Neurological Disease
    CR 665 (JNJ 38488502) is a peripherally selective κ-opioid agonist. CR 665 can activate the kappa opioid receptor with EC50 value of 10.9 nM. CR 665 can be used for the research of peripheral pain .
    CR 665
  • HY-103354
    Proglumide sodium
    1 Publications Verification

    Cholecystokinin Receptor Neurological Disease Endocrinology Cancer
    Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities .
    Proglumide sodium
  • HY-172429A

    ORIC-114 hemihydrate

    EGFR Neurological Disease Cancer
    Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
    Enozertinib hemihydrate
  • HY-122026

    PF-367

    GSK-3 Neurological Disease
    PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively .
    PF-04802367
  • HY-153615

    mGluR Neurological Disease
    CVN636 is a potent, orally active and selective mGluR7 allosteric agonist with an EC50 value of 7 nM for hu mGluR7. CVN636 has central nervous system (CNS) permeability .
    CVN636
  • 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-B0971

    Prophenpyridamine maleate; Tripoton maleate

    Histamine Receptor Apoptosis Inflammation/Immunology Endocrinology
    Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
    Pheniramine maleate
  • HY-13011S

    CH5424802-d8; RO5424802-d8; AF802-d8

    Isotope-Labeled Compounds Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib-d8
  • HY-145777

    Methionine Adenosyltransferase (MAT) Neurological Disease Cancer
    AGI-43192 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that limitedly penetrates the blood-brain barrier. AGI-43192 exhibits inhibitory activitity against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC50s of 32 and 14 nM. AGI-43192 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-43192 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .
    AGI-43192
  • HY-145778

    Methionine Adenosyltransferase (MAT) Neurological Disease Cancer
    AGI-41998 is a potent and orally active inhibitor of methionine adenosyltransferase 2A (MAT2A) that effectively penetrates the blood-brain barrier. AGI-41998 exhibits inhibitory activities against MAT2A and S-adenosyl methionine (SAM) in HCT-116 MTAP-null cells with IC50s of 22 nM and 34 nM. AGI-41998 can significantly inhibit the proliferation of HCT-116 cells and tumor growth. AGI-41998 can be used to study the role of SAM regulation in the central nervous system (CNS) and colon cancer .
    AGI-41998
  • HY-172182

    VU6011887

    Potassium Channel Neurological Disease
    ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.
    ONO-2920632
  • HY-14550A

    Phosphodiesterase (PDE) Others
    PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders .
    PDE10-IN-5
  • HY-164307

    BLU 451; LNG-451

    EGFR Cancer
    Pebezertinib (BLU 451) is an orally active inhibitor for EGFR. Pebezertinib exhibits the ability to penetrate the central nervous system (CNS). Pebezertinib can be used for research about non-small cell lung cancer carrying EGFR exon 20 insertion .
    Pebezertinib
  • HY-13011AR

    CH5424802 Hydrochloride (Standard); RO5424802 Hydrochloride (Standard); AF-802 Hydrochloride (Standard)

    Anaplastic lymphoma kinase (ALK) Reference Standards Cancer
    Alectinib (Hydrochloride) (Standard) is the analytical standard of Alectinib (Hydrochloride). This product is intended for research and analytical applications. Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
    Alectinib Hydrochloride (Standard)
  • HY-137952

    Potassium Channel TRP Channel Neurological Disease
    NS8593 is an SK channel (small conductance Ca 2+-activated K+ channels) inhibitor. NS8593 reversibly inhibited recombinant SK3-mediated currents (human SK3 and rat SK3). NS8593 inhibits all the SK1-3 subtypes Ca 2+-dependently (Kd = 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+). NS8593 does not affect the Ca 2+-activated K channels of intermediate and large conductance (hlk and hBK channels, respectively). NS8593 can also inhibit TRPM7 (melastatin-related TRP cation channel 7) (IC50 = 1.6 mM). NS8593 can be used for the study of central nervous system (CNS) related diseases .
    NS8593
  • HY-P3800

    Neurokinin Receptor Neurological Disease Endocrinology
    [Glp5] Substance P (5-11) is an octapeptide. [Glp5] Substance P (5-11) is one of the main substance P fragments in rat central nervous system (CNS). [Glp5] Substance P (5-11) locally modulates dopamine release in rat striatum .
    [Glp5] Substance P (5-11)
  • 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-145887

    Bcr-Abl Cancer
    BCR-ABL1-IN-1 (Example 74) is the inhibitor for ABL1 (64-515) with IC50 of 8.7 nM. BCR-ABL1-IN-1 can be used in research on diseases related to the central nervous system (CNS) .
    BCR-ABL1-IN-1
  • HY-B0971A

    Prophenpyridamine; Tripoton; Pheniramine solution

    Histamine Receptor Apoptosis Inflammation/Immunology Cancer
    Pheniramine (Prophenpyridamine;Tripoton) is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine displays antitumor effect and induces leukemia cells apoptosis. Pheniramine is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects .
    Pheniramine
  • HY-W739056

    Isotope-Labeled Compounds Biochemical Assay Reagents Neurological Disease
    SAMe-1,4-Butanedisulfonate-d3 is the deuterium labeled SAMe-1,4-Butanedisulfonate (HY-W105505). 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-d3
  • HY-178871

    Orexin Receptor (OX Receptor) Neurological Disease
    OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research .
    OX2-2303
  • HY-170973

    Opioid Receptor
    KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
    KOR agonist 4
  • HY-19699

    NAAM; 1-Naphthaleneacetamide; α-Naphthylacetamide

    Environmental Pollutants Phytohormone Neurological Disease Endocrinology
    1-Naphthylacetamide is an orally active nonsteroidal anti-inflammatory agent (NAIA) and also an indole-type auxin plant growth regulator. 1-Naphthylacetamide inhibits inflammatory response-related pathways and modulates plant hormone signaling, exhibiting anti-inflammatory, local anesthetic, antispasmodic, analgesic, and diuretic activities. 1-Naphthylacetamide promotes plant cell expansion, differentiation, and fruit enlargement. Additionally, 1-Naphthylacetamide induces central nervous system (CNS) depression in mice, characterized by reduced spontaneous activity, decreased irritability, decreased muscle tone, and attenuated ear-cuff reflex, ipsilateral flexor reflex, and corneal reflex [1][2].
    1-Naphthylacetamide
  • HY-170771

    GABA Receptor Neurological Disease
    α5-GABAA receptor modulator 1 (Compound A-4) is a silencing allosteric modulator (SAM) specifically targeting the a5 subunit of the GABAA receptor, suitable for research into central nervous system (CNS) disorders .
    α5-GABAA receptor modulator 1
  • HY-B0740S

    MK130-d3 hydrochloride

    Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
    Cyclobenzaprine-d3 hydrochloride
  • HY-160446

    Epigenetic Reader Domain Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Bet-in-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor. BET-IN-24 can be used in the study of virology, heart failure, inflammation, central nervous system (CNS) diseases and many cancers
    BET-IN-24
  • HY-163855

    Sodium Channel GABA Receptor Neurological Disease
    KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia .
    KGP-25
  • HY-116819A

    GCGR Metabolic Disease
    VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
    VU0453379 hydrochloride
  • HY-175372

    Histamine Receptor Neurological Disease
    H3R antagonist 7 (compounds 4) is a histamine subtype 3 receptor (H3R) antagonist with a Ki of 3.15 nM. H3R antagonist 7 is a potential PET radioligand for the study of central nervous system (CNS) diseases .
    H3R antagonist 7
  • HY-122647

    VU0652957; VU2957

    mGluR Neurological Disease
    Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .
    Valiglurax

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