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Results for "

CNS

" in MCE Product Catalog:

220

Inhibitors & Agonists

5

Screening Libraries

1

Fluorescent Dye

20

Peptides

1

Inhibitory Antibodies

11

Natural
Products

15

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-101809
    CNS-5161 hydrochloride

    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.
  • HY-110097
    Aptiganel hydrochloride

    CNS 1102

    iGluR Neurological Disease
    Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
  • HY-N2321
    Salsolinol-1-carboxylic acid

    Others Neurological Disease
    Salsolinol-1-carboxylic acid is an endogenous alkaloid in the central nervous system (CNS).
  • HY-B0250A
    Lamivudine salicylate

    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.
  • HY-P2457
    rCRAMP (rat)

    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.
  • HY-101281A
    (Rac)-VU 6008667

    mAChR Neurological Disease
    (Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
  • HY-144764
    5-HT1A antagonist 1

    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.
  • HY-132981
    Lu AF27139

    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.
  • HY-15722
    SB-222200

    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.
  • HY-B0250
    Lamivudine

    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.
  • HY-122138
    VU6010572

    mGluR Neurological Disease
    VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant.
  • HY-14905
    Uridine triacetate

    Tri-O-acetyl uridine

    Others Neurological Disease
    Uridine triacetate (Tri-O-acetyl uridine) is an orally active prodrug 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).
  • HY-110191
    VU0469650

    mGluR Cancer Neurological Disease
    VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM.
  • HY-147405
    Tinlorafenib

    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.
  • HY-133554
    ASK1-IN-1

    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).
  • HY-101281
    VU 6008667

    mAChR Neurological Disease
    VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration.
  • HY-147639
    Cav 2.2/3.2 blocker 1

    Calcium Channel Neurological Disease
    Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC50 values of 78 μM and 80 μM against Cav2.2 and Cav3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS.
  • HY-139279
    TPX-0131

    Anaplastic lymphoma kinase (ALK) Cancer
    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). TPX-0131 has strong antitumor activities.
  • HY-109189
    Rezivertinib

    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.
  • HY-118158
    FAAH/MAGL-IN-4

    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.
  • HY-10974
    MK-0752

    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.
  • HY-144372
    TRPV1 antagonist 3

    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.
  • HY-144696
    Dyrk1A/α-synuclein-IN-2

    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.
  • HY-147657
    GABAA receptor modulator-2

    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.
  • HY-131068
    BACE-1 inhibitor 2

    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.
  • HY-138879B
    CP-601932

    (1S,5R)-CP-601927

    nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS.
  • HY-111263
    NIAD-4

    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.
  • HY-12776
    GSK805

    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.
  • HY-15043
    ELN-441958

    Bradykinin Receptor Endocrinology Inflammation/Immunology
    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.
  • HY-144695
    Dyrk1A/α-synuclein-IN-1

    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.
  • HY-131181
    LEI-401

    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.
  • HY-145695
    Dual AChE-MAO B-IN-1

    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.
  • HY-10968
    CYM5442

    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).
  • HY-10968A
    CYM5442 hydrochloride

    LPL Receptor Neurological Disease
    CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS).
  • HY-119974
    Caracemide

    NSC-253272

    DNA/RNA Synthesis Bacterial Cancer Infection
    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.
  • HY-18679
    TC-N 22A

    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.
  • HY-124754
    BTRX-335140

    CYM-53093

    Opioid Receptor Metabolic Disease Neurological Disease
    BTRX-335140 (CYM-53093) 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. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 distributes well into the CNS and can be used for the research of neuropathy.
  • HY-N8441
    Neriifolin

    17β-Neriifolin

    Na+/K+ ATPase Apoptosis Cancer Inflammation/Immunology
    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.
  • HY-122697
    ML418

    Potassium Channel Endocrinology Neurological Disease Cardiovascular Disease
    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.
  • HY-150503
    KH-259

    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.
  • HY-116016
    Etilevodopa

    L-DOPA ethyl ester; Levodopa ethyl ester

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester), an ethyl-ester prodrug 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 prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-116016A
    Etilevodopa hydrochloride

    L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride

    Dopamine Receptor Drug Metabolite Neurological Disease
    Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester prodrug 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 prodrug as it facilitates CNS penetration and delivers dopamine.
  • HY-110146
    XAP044

    mGluR Neurological Disease
    XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms.
  • HY-110216
    5J-4

    CRAC Channel Inflammation/Immunology
    5J-4 is a potent CRAC inhibitor. 5J-4 decreases the numbers of infiltrated mononuclear cell into the CNS, and significantly decreases the population of infiltrated CD4+ population. 5J-4 reduces the symptoms and delayed the onset of EAE (experimental autoimmune encephalomyelitis) in mouse model of inflammation.
  • HY-125021
    2BAct

    Eukaryotic Initiation Factor (eIF) Neurological Disease
    2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB (HY-12495).
  • HY-145838
    AAK1-IN-4

    Others Neurological Disease
    AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 4.6 nM, Filt Ki of 0.9 nM, and cell IC50 of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
  • HY-145839
    AAK1-IN-5

    Others Neurological Disease
    AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
  • HY-128575
    BNC375

    nAChR Neurological Disease
    BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-drug like properties and clinical candidate potential. .
  • HY-108460
    A-784168

    TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
  • HY-103354
    Proglumide sodium

    Cholecystokinin Receptor Cancer Endocrinology Neurological Disease
    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.
  • HY-B1330
    Proglumide

    Cholecystokinin Receptor Cancer Endocrinology Neurological Disease
    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.
  • HY-144827
    AM8936

    Cannabinoid Receptor Neurological Disease Metabolic Disease
    AM8936 acts as a balanced and potent cannabinoid receptor type-1 (CB1) agonist in functional assays (EC50s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits high affinity for rat CB1 (rCB1) with Ki of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc.
  • HY-144074
    LRRK2-IN-4

    LRRK2 Neurological Disease
    LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.
  • HY-103354A
    Proglumide hemicalcium

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

    PKC HIV Bacterial Cancer Infection Inflammation/Immunology Neurological Disease
    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.
  • HY-14951
    Firategrast

    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.
  • HY-147999
    GlcN-6-P Synthase-IN-1

    Bacterial Fungal Cytochrome P450 Infection
    GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform.
  • HY-105685
    SRX246

    Vasopressin Receptor Neurological Disease
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-19978
    RO-3

    P2X Receptor Neurological Disease
    RO-3 is a potent, CNS-penetrant, and orally active P2X3 and P2X2/3 antagonist with pIC50s of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. RO-3 shows selectivity for P2X3 and P2X2/3 over all other functional homomultimeric P2X receptors (IC50 >10 μM at P2X1,2,4,5,7).
  • HY-W001601
    Budipine

    iGluR Neurological Disease
    Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease.
  • HY-10035
    TTA-P2

    T-Type calcium channel inhibitor

    Calcium Channel Neurological Disease
    TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
  • HY-B0653
    Levobupivacaine

    (S)-(-)-Bupivacaine

    Sodium Channel Ferroptosis Cancer Neurological Disease
    Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local anaesthetic. Levobupivacaine exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-B0653A
    Levobupivacaine hydrochloride

    (S)-(-)-Bupivacaine monohydrochloride

    Sodium Channel Ferroptosis Neurological Disease Cancer
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local anaesthetic. Levobupivacaine hydrochloride exerts anaesthetic and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
  • HY-120184
    VU0467485

    AZ13713945

    mAChR Neurological Disease
    VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
  • HY-N2309
    Kainic acid

    EAAT2 Neurological Disease
    Kainic acid is a potent agonist at excitatory amino acid receptor subtypes in the CNS.
  • HY-N2072
    Transcrocetin

    trans-Crocetin

    iGluR Endogenous Metabolite Cancer
    Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity. Transcrocetin (trans-Crocetin) is capable of crossing the blood-brain barrier and reach the central nervous system (CNS).
  • HY-B0740
    Cyclobenzaprine hydrochloride

    MK130 hydrochloride

    5-HT Receptor Neurological Disease
    Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
  • HY-115726
    FRM-024

    γ-secretase Neurological Disease
    FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.
  • HY-A0168
    Regadenoson

    CVT-3146

    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-U00076
    MK-0249

    Histamine Receptor Neurological Disease Endocrinology
    MK-0249 (Compound 1) is a potent, selective and orally active histamine H3 receptor antagonist, with an IC50 of 1.7 nM for human H3.
  • HY-U00155
    NCI172112

    NSC172112; NSC268497

    DNA Alkylator/Crosslinker Cancer
    NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
  • HY-B0194A
    Tizanidine hydrochloride

    Adrenergic Receptor Cancer Neurological Disease Endocrinology
    Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-B0194
    Tizanidine

    Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-117632
    ABX-1431

    MAGL Neurological Disease
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • HY-N3193
    Neritaloside

    Others Neurological Disease
    Neritaloside could be isolated from nerium oleander. Neritaloside has central nervous system (CNS) depressant effect[2.
  • HY-N2428
    N-(3-Methoxybenzyl)Palmitamide

    FAAH Neurological Disease
    N-(3-Methoxybenzyl)Palmitamide is a promising inhibitor of FAAH for the treatment of pain, inflammation and CNS degenerative disorders.
  • HY-17573A
    Carbetocin acetate

    Oxytocin Receptor Endocrinology Neurological Disease
    Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
  • HY-17573
    Carbetocin

    Oxytocin Receptor Endocrinology Neurological Disease
    Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
  • HY-130121
    MK-8719

    Others Neurological Disease
    MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration.
  • HY-15050
    KCL-440

    PARP Inflammation/Immunology Neurological Disease
    KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1.
  • HY-Y0966
    Glycine

    Endogenous Metabolite iGluR Neurological Disease
    Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-14758
    Adipiplon

    NG2-73

    GABA Receptor Neurological Disease
    Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the treatment of a variety of central nervous system (CNS) disorders.
  • HY-14550A
    PDE10-IN-5

    Phosphodiesterase (PDE) Others
    PDE10-IN-5 is a phosphodiesterase 10 (PDE 10) inhibitor, can be used for researching certain central nervous system (CNS) disorders.
  • HY-109055
    Elenbecestat

    E2609

    Beta-secretase Neurological Disease
    Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
  • HY-108463
    A-967079

    TRP Channel Inflammation/Immunology
    A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
  • HY-137061
    AZ-GHS-22

    GHSR Metabolic Disease
    AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM).
  • HY-12813
    PDE10-IN-1

    Phosphodiesterase (PDE) Neurological Disease
    PDE10-IN-1 is a potent PDE10-IN-1 inhibitor extracted from Patent WO 2013192273 A1, for treating CNS and metabolic disorders.
  • HY-U00180
    KF21213

    Adenosine Receptor Neurological Disease
    KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM).
  • HY-P0201
    Substance P

    Neurokinin P

    Neurokinin Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-112286
    PI3Kγ inhibitor 2

    PI3K Inflammation/Immunology
    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  • HY-B0740S
    Cyclobenzaprine-d3 hydrochloride

    MK130-d3 hydrochloride

    5-HT Receptor Neurological Disease
    Cyclobenzaprine-d3 (MK130-d3) hydrochloride is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
  • HY-16617
    Auglurant

    VU0424238

    mGluR Neurological Disease
    Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration.
  • HY-U00123A
    Guanoxabenz hydrochloride

    Hydroxyguanabenz hydrochloride

    Adrenergic Receptor Neurological Disease
    Guanoxabenz (Hydroxyguanabenz) hydrochloride is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.
  • HY-U00123
    Guanoxabenz

    Hydroxyguanabenz

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Guanoxabenz is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.
  • HY-106578
    Quinupramine

    LM 208

    Others Neurological Disease
    Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
  • HY-B0194S
    Tizanidine-d4

    Adrenergic Receptor Neurological Disease Endocrinology Cancer
    Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
  • HY-107982
    VU6005649

    mGluR Neurological Disease
    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  • HY-101789
    Nav1.7-IN-3

    Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  • HY-Y0966S10
    Glycine-d3

    Endogenous Metabolite iGluR Cancer
    Glycine-d3 is the deuterium labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-Y0966S8
    Glycine-d5

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-d5 is the deuterium labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-Y0966S1
    Glycine-d2

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-d2 is the deuterium labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-145607
    Zagociguat

    Guanylate Cyclase Cardiovascular Disease
    Zagociguat is the stimulator of soluble guanylate cyclase. Zagociguat increases nitric oxide (NO) signaling leading to an increase in cyclic guanosine monophosphate production. Zagociguat has the potential for the research of noncentral nervous system (CNS) disorders.
  • HY-119943
    PF-06256142

    Dopamine Receptor Neurological Disease
    PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
  • HY-108710
    VU0650786

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-123481
    JNJ-42253432

    P2X Receptor Metabolic Disease
    JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
  • HY-107790
    5-Methoxyflavone

    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.
  • HY-101653
    MHP 133

    Cholinesterase (ChE) mAChR 5-HT Receptor Neurological Disease
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  • HY-Y0966S2
    Glycine-2-13C

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-13C is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-P0201A
    Substance P TFA

    Neurokinin P TFA

    Neurokinin Receptor Endogenous Metabolite Endocrinology Neurological Disease Cancer
    Substance P TFA (Neurokinin P TFA) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-109527
    5-HT7 agonist 1

    5-HT Receptor Neurological Disease
    5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
  • HY-100483
    A-804598

    P2X Receptor Cancer
    A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
  • HY-122015
    ASP2905

    Potassium Channel Neurological Disease
    ASP2905 is a potent and selective potassium channel Kv12.2 inhibitor encoded by the Kcnh3/BEC1 gene. ASP2905 can cross the blood-brain barrier and has antipsychotic activities.
  • HY-146101
    NMDA receptor antagonist 5

    iGluR Neurological Disease
    NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research.
  • HY-122381
    Kyotorphin

    Bacterial Endogenous Metabolite Neurological Disease
    Kyotorphin is an endogenou neuroactive dipeptide with analgesic properties. Kyotorphin possesses anti-inflammatory and antimicrobial activity. Kyotorphin levels in cerebro-spinal fluid correlate negatively with the progression of neurodegeneration in Alzheimer's Disease patients.
  • HY-Y0966S4
    Glycine-1-13C

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-1-13C is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-116819
    VU0453379

    GCGR Metabolic Disease
    VU0453379 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.
  • HY-100376
    CPI-1189

    TNF Receptor Infection Neurological Disease
    CPI-1189 is a TNF-α release inhibitor with antioxidant and neuroprotective properties. CPI-1189 is used for researches of HIV-associated neurotoxicity and thus is a candidate for neuroprotective therapy in humans suffered from HIV-associated CNS disease.
  • HY-101116
    GLP-1R Antagonist 1

    GCGR Metabolic Disease
    GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
  • HY-B0770
    Artemotil

    β-Arteether; (+)-Arteether; Arteether

    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.
  • HY-Y0966S3
    Glycine-13C2

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-13C2 is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-Y0966S
    Glycine-15N

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-15N is the 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-120813
    ARN 077

    URB913

    Others Inflammation/Immunology
    ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.
  • HY-147821
    CB1-IN-2

    Cannabinoid Receptor Metabolic Disease
    CB1-IN-2 (Compound 4g) is a selective CB1 inhibitor with an IC50 of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant.
  • HY-Y0966S9
    Glycine-15N,d2

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-15N,d2 is the deuterium and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-129586
    AT-007

    Aldose Reductase Metabolic Disease
    AT-007 is an orally active central nervous system (CNS) penetrant Aldose Reductase inhibitor for treatment of Galactosemia with an IC50 value of 100 pM. AT-007 reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.
  • HY-151592
    Anticancer agent 91

    Others Cancer
    Anticancer agent 91 is a benzothiazole-2-thiophene S-glycoside derivative with antitumor and antiviral activity. Anticancer agent 91 has high inhibition against the two cell line from CNS cancer (SF-539 and SNB-75).
  • HY-17595
    Mebendazole

    Parasite Apoptosis Microtubule/Tubulin Infection Cancer
    Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration.
  • HY-145778
    AGI-41998

    Somatostatin Receptor Neurological Disease
    AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-P2546
    Biotin-Substance P

    Neurokinin Receptor Neurological Disease
    Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-12650
    Mirogabalin

    DS5565

    Calcium Channel Neurological Disease
    Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
  • HY-145777
    AGI-43192

    Somatostatin Receptor Cancer Neurological Disease
    AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.
  • HY-15344A
    (S,S)-BD-AcAc 2

    (S,S)-Ketone Ester

    Others Neurological Disease
    (S,S)-BD-AcAc 2 ((S,S)-Ketone Ester) is a (S,S)-enantiomer of BD-AcAc 2. BD-AcAc 2 elevates the AcAc and acetone levels, thereby produces sustained ketosis and significantly delays central nervous system oxygen toxicity (CNS-OT) seizures.
  • HY-147399
    5-HT7 agonist 2

    5-HT Receptor Neurological Disease
    5-HT7 agonist 2 is a potent 5-HT7 receptor agonist with an IC50 value of 28.7 nM. 5-HT7 agonist 2 can be used for research of central nervous system (CNS) disorders.
  • HY-15196
    TAK-285

    EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-19838
    JNJ-63533054

    GPR139 Neurological Disease
    JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB).
  • HY-150640
    Rho-Kinase-IN-2

    ROCK Neurological Disease
    Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.
  • HY-P3800
    [Glp5] Substance P (5-11)

    Neurokinin Receptor Endocrinology Neurological Disease
    [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.
  • HY-Y0966S7
    Glycine-2-13C,15N

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-2-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-Y0966S6
    Glycine-13C2,15N

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-13C2,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-Y0966S5
    Glycine-1-13C,15N

    Endogenous Metabolite iGluR Neurological Disease
    Glycine-1-13C,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
  • HY-112340
    TM38837

    Cannabinoid Receptor Metabolic Disease
    TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.
  • HY-120111
    MW-150

    MW01-18-150SRM

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-P1333
    Dynorphin A

    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.
  • HY-145830
    AC1-IN-1

    Adenylate Cyclase Neurological Disease
    AC1-IN-1 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC50 of 0.54 µM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity.
  • HY-146230
    VEGFR-2-IN-26

    VEGFR Cancer
    VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells.
  • HY-136109
    SEP-363856 hydrochloride

    SEP-856 hydrochloride

    5-HT Receptor Neurological Disease
    SEP-363856 hydrochloride (SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia.
  • HY-12150
    CCMI

    AVL-3288; UCI-4083

    nAChR Neurological Disease
    CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
  • HY-145086
    R-PSOP

    Others Metabolic Disease
    R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders.
  • HY-136109A
    SEP-363856

    SEP-856

    5-HT Receptor Neurological Disease
    SEP-363856 (SEP-856), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the study of schizophrenia.
  • HY-101418
    JNJ-47965567

    P2X Receptor Neurological Disease
    JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.
  • HY-101333
    CPPG

    (RS)-CPPG

    mGluR Neurological Disease
    CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-107479
    (R)-JNJ-31020028

    Neuropeptide Y Receptor Neurological Disease
    (R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
  • HY-16725
    Lemborexant

    E-2006

    Orexin Receptor (OX Receptor) Neurological Disease
    Lemborexant (E-2006) is a reversible, competitive and orally active dual antagonist of the orexin OX1 and OX2 receptors with IC50 values of 6.1 nM and 2.6 nM, respectively. Lemborexant can be treated insomnia.
  • HY-16100
    BI 99179

    Fatty Acid Synthase (FASN) Cancer Metabolic Disease
    BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
  • HY-128772
    XPC-6444

    Sodium Channel Neurological Disease
    XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.
  • HY-130252
    YQ128

    NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
  • HY-151589
    HCVcc-IN-2

    Virus Protease Cancer Infection
    HCVcc-IN-2 is a benzothiazole-2-thiophene S-glycoside derivative with antitumor and antiviral activity. HCVcc-IN-2 has high inhibition against the three cell line from CNS cancer (SF-539 and SNB-75), colon cancer (HCT-116), and renal cancer (A498).
  • HY-P1333A
    Dynorphin A TFA

    Opioid Receptor Apoptosis Caspase Endogenous Metabolite Neurological Disease
    Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA 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 TFA can induce neuronal death, and can be used in the research of neurological disease.
  • HY-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
  • HY-17377
    Vicriviroc maleate

    SCH-417690 maleate; SCH-D maleate

    CCR HIV Infection Endocrinology
    Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).
  • HY-146662
    HPGDS inhibitor 3

    PGE synthase Inflammation/Immunology
    HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
  • HY-120111A
    MW-150 hydrochloride

    MW01-18-150SRM hydrochloride

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • 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.
  • HY-13011
    Alectinib

    CH5424802; RO5424802; AF802

    Anaplastic lymphoma kinase (ALK) Cancer
    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.
  • HY-W007524
    2-Aminoquinoline

    2-Quinolinamine

    NO Synthase Orthopoxvirus Infection Neurological Disease
    2-Aminoquinoline (2-Quinolinamine) is a promising compound as bioavailable nNOS inhibitor but suffers from low human nNOS inhibition, low selectivity versus human eNOS, and significant binding to other CNS targets. 2-Aminoquinoline exhibits antiviral activity against the vaccinia virus. 2-Aminoquinoline has the potential for the research of antineurodegenerative agents.
  • HY-148115
    S1p receptor agonist 2

    LPL Receptor Inflammation/Immunology
    S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders.
  • HY-115460
    AER-271

    Aquaporin Neurological Disease Cardiovascular Disease
    AER-271, a phosphonate prodrug derivative of AER-270, is an aquaporin-4 (AQP4) inhibitor for the research of acute ischemic stroke.
  • HY-107663
    MIF-1

    Pro-Leu-Gly-NH2; Melanostatin

    Dopamine Receptor Neurological Disease
    MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
  • HY-13011A
    Alectinib Hydrochloride

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    Anaplastic lymphoma kinase (ALK) Cancer
    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.
  • HY-120111B
    MW-150 dihydrochloride dihydrate

    MW01-18-150SRM dihydrochloride dihydrate

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-144608
    Mu opioid receptor antagonist 3

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD).
  • HY-136109B
    (Rac)-SEP-363856

    (Rac)-SEP-856

    5-HT Receptor Neurological Disease
    (Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856(SEP-856), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the treatment of schizophrenia.
  • HY-14472
    Tesofensine

    NS-2330

    Dopamine Transporter Serotonin Transporter Metabolic Disease
    Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.
  • HY-13011S1
    Alectinib-d6

    CH5424802-d6; RO5424802-d6; AF802-d6

    Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d6 is 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.
  • HY-105066
    Davunetide

    Microtubule/Tubulin Amyloid-β Neurological Disease
    Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.
  • HY-111191
    ONO-2952

    Adrenergic Receptor Neurological Disease
    ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
  • HY-130795
    GSK-3β inhibitor 2

    GSK-3 Neurological Disease
    GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
  • HY-100815B
    (RS)-AMPA

    (±)-AMPA

    iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors.
  • HY-100815D
    (RS)-AMPA monohydrate

    (±)-AMPA monohydrate

    iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors.
  • HY-150639
    Everafenib

    Raf Cancer
    Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma.
  • HY-144609
    Mu opioid receptor antagonist 4

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD).
  • HY-144607
    Mu opioid receptor antagonist 2

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD).
  • HY-107663A
    MIF-1 TFA

    Pro-Leu-Gly-NH2 TFA; Melanostatin TFA

    Dopamine Receptor Neurological Disease
    MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
  • HY-12596
    JNJ-26489112

    Calcium Channel Sodium Channel Potassium Channel Neurological Disease
    JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-type Ca 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM).
  • HY-108831
    Natalizumab

    Integrin Inflammation/Immunology
    Natalizumab is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.
  • HY-112831
    Osoresnontrine

    BI-409306

    Phosphodiesterase (PDE) Neurological Disease
    Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.
  • HY-119939
    CHDI-390576

    HDAC Cancer
    CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
  • HY-128879
    VP3.15

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-B0193A
    Prazosin hydrochloride

    Adrenergic Receptor Autophagy Cardiovascular Disease Endocrinology Cancer
    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
  • HY-128879A
    VP3.15 dihydrobromide

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-145845
    HDAC1/MAO-B-IN-1

    HDAC Monoamine Oxidase Neurological Disease
    HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.
  • HY-122347A
    Orvepitant maleate

    GW823296 maleate

    Neurokinin Receptor Neurological Disease
    Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.
  • HY-13011S
    Alectinib-d8

    CH5424802-d8; RO5424802-d8; AF802-d8

    Anaplastic lymphoma kinase (ALK) Cancer
    Alectinib-d8 (CH5424802-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.
  • HY-136207
    TC-2559 difumarate

    nAChR Neurological Disease
    TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
  • HY-12501A
    ITI-214

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
  • HY-107691
    GR 159897

    Neurokinin Receptor Cancer Endocrinology Neurological Disease
    GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK2) receptor antagonist. GR 159897 has little or no affinity for NK1 and NK3 receptors. GR 159897 inhibits binding of [ 3H]GR100679 to human NK2 (hNK2)-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects.
  • HY-103309A
    ML218 hydrochloride

    Calcium Channel Neurological Disease
    ML218 hydrochloride is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier.
  • HY-103309
    ML218

    Calcium Channel Neurological Disease
    ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier.
  • HY-100370
    MRK-016

    GABA Receptor Cancer
    MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
  • HY-12501
    ITI-214 free base

    Phosphodiesterase (PDE) Neurological Disease
    ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
  • HY-110053
    Tandospirone hydrochloride

    SM-3997 hydrochloride

    5-HT Receptor Neurological Disease
    Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms.
  • HY-14558
    Tandospirone

    SM-3997

    5-HT Receptor Neurological Disease
    Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
  • HY-124619
    GPI-1046

    FKBP HIV Infection Neurological Disease
    GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-122026
    PF-04802367

    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.
  • HY-12345
    ML365

    Potassium Channel Cardiovascular Disease
    ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels.
  • HY-136459
    NMDA receptor antagonist 2

    iGluR Neurological Disease
    NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
  • HY-13637B
    Ganciclovir hydrate

    BW-759 hydrate; 2'-Nor-2'-deoxyguanosine hydrate

    CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Cancer Infection
    Ganciclovir (BW 759) hydrate, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir hydrate also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir hydrate inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir hydrate has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
  • HY-151094
    FTEAA

    Monoamine Oxidase Neurological Disease
    FTEAA is a 4-styrylpiperidine inhibitor. FTEAA exhibits potent inhibitory effect towards both monoamine oxidase with IC50s of 0.52 μM (MAO-A), 1.02 μM (MAO-B), respectively. MAO inhibitors can be used for cardiovascular, neurological and oncological disorders research.
  • HY-13637
    Ganciclovir

    BW 759; 2'-Nor-2'-deoxyguanosine

    CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
  • HY-13637A
    Ganciclovir sodium

    BW 759 sodium; 2'-Nor-2'-deoxyguanosine sodium

    CMV HSV Antibiotic Nucleoside Antimetabolite/Analog Infection Cancer
    Ganciclovir (BW 759) sodium, a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir sodium also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir sodium inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir sodium has an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.
  • HY-124832
    δ-Secretase inhibitor 11

    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.
  • HY-N0067
    γ-Aminobutyric acid

    4-Aminobutyric acid

    GABA Receptor Endogenous Metabolite Neurological Disease
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.
  • HY-147864
    c-Fms-IN-12

    c-Fms c-Kit Apoptosis Cancer
    c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.
  • HY-147409
    Ulecaciclib

    CDK Cancer
    Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics.
  • HY-147377
    N-Salicyloyltryptamine

    Calcium Channel ERK Potassium Channel Guanylate Cyclase NF-κB Inflammation/Immunology Neurological Disease
    N-Salicyloyltryptamine acts on voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor. N-Salicyloyltryptamine inhibits K + currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect -.