2. Neurological Disease

Neurological Disease

Neurological Disease

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A range of neurological disorders, including epilepsy and dystonia, may involve dysfunctional intracortical inhibition, and may respond to treatments that modify it. Parkinson’s is a neurodegenerative disease characterized by increased activity of GABA in basal ganglia and the loss of dopamine in nigrostriatum, associated with rigidity, resting tremor, gait with accelerating steps, and fixed inexpressive face. Neurological deficits, along with neuromuscular involvement, are characteristic of mitochondrial disease, and these symptoms can have a dramatic impact on patient quality of life. Neurological features may be manifold, ranging from neural deafness, ataxia, peripheral neuropathy, migraine, seizures, stroke‐like episodes and dementia and depend on the part of the nervous system affected.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-178871
    OX2-2303 1607428-33-0
    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-178920
    α-Synuclein-IN-17 676458-63-2 98.00%
    α-Synuclein-IN-17 (Compound 10) is an α-Synuclein inhibitor, with an IC50 value of 9 μM. α-Synuclein-IN-17 exhibits potent inhibitory activity against both in-vitro assembled asyn fibrils and LBD brain tissue-amplified asyn fibrils. α-Synuclein-IN-17 can be used for the study of Parkinson's disease (PD) and Lewy Body Disease (LBD).
    α-Synuclein-IN-17
  • HY-178927
    Tau-aggregation-IN-4
    Tau-aggregation-IN-4 is a Tau-aggregation inhibitor (EC50 = 2.99 μM). Tau-aggregation-IN-4 can be used for the study of neurodegenerative disorders such as Alzheimer’s and Pick’s diseases.
    Tau-aggregation-IN-4
  • HY-178939
    EGFR-IN-181
    EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases.
    EGFR-IN-181
  • HY-178943
    Neuroprotective agent 15 2476614-40-9
    Neuroprotective agent 15 (Compound 3e) is a neuroprotective agent. Neuroprotective agent 15 is a selective butyrylcholinesterase (BChE) inhibitor, with IC50 values of 2.6 and 114.3 μM for BChE and AChE respectively. Neuroprotective agent 15 has cannabinoid CB2 receptor (CB2 receptor) agonistic activity. Neuroprotective agent 15 can reduce cell death, LDH release and Caspase-3/7 activity, and inhibit apoptosis. Neuroprotective agent 15 can reduce the formation of superoxide free radicals, maintain cell morphology, and significantly lower oxidative stress levels. Neuroprotective agent 15 can be used in the research of neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease.
    Neuroprotective agent 15
  • HY-178945
    KOR agonist 7
    KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a Ki of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (Ki = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.
    KOR agonist 7
  • HY-178963
    Nav1.2-IN-2 7469-49-0 99.82%
    Nav1.2-IN-2 is a Nav1.2 inhibitor with a human IC50 of 0.18 μM. Nav1.2-IN-2 preferentially binds to the inactivated state of Nav1.2, reduces window current, suppresses neuronal depolarization and action potential generation. Nav1.2-IN-2 suppresses Veratridine (HY-N6691)-induced Ca2+ influx. Nav1.2-IN-2 can be used for the research of epilepsy.
    Nav1.2-IN-2
  • HY-178969
    GZD-257
    GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM).
    GZD-257
  • HY-179004
    ONO-9517601 2640753-22-4
    ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.
    ONO-9517601
  • HY-179005
    ONO-7927846 2640753-27-9 98%
    ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders.
    ONO-7927846
  • HY-179008
    5-HT2CR agonist 2 2841457-05-2
    5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT2CR agonist, with an EC50 of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity.
    5-HT2CR agonist 2
  • HY-179014
    OGG1 activator-1 98%
    OGG1 activator-1 (Compound 30) is a selective 8-oxoguanine DNA glycosylase-1 (OGG1) activator with an AC50 value of 0.58 μM. OGG1 activator-1 does not activate nor inhibit the key downstream repair enzyme APE1, and shows > 150-fold selectivity for the activation effect on OGG1. OGG1 activator-1 exhibits extremely high metabolic stability and almost no cytotoxicity. OGG1 activator-1 can be used for the study of oxidative stress-related diseases (such as neurodegenerative diseases, fibrotic diseases, cancer, inflammation, etc.).
    OGG1 activator-1
  • HY-179019
    HDAC-IN-94 98%
    HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC50 = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.
    HDAC-IN-94
  • HY-179027
    LDH-IN-5 2768522-31-0
    LDH-IN-5 is a Lactate Dehydrogenase (LDH) inhibitor with neuroprotective activity. LDH-IN-5 can inhibit cell apoptosis, reduce ROS, MDA production and increases superoxide dismutase (SOD) activity. LDH-IN-5 can be used for the research of neurological disease, such as ischemic stroke.
    LDH-IN-5
  • HY-179037
    NecroX-2 1120333-38-1
    NecroX-2 is a potent inhibitor of caspase-independent necrosis. NecroX-2 exhibits antioxidant activity by scavenging DPPH radicals and peroxynitrite. NecroX-2 inhibits t-BHP-induced mitochondrial ROS/RNS generation, and protects t-BHP and Doxorubicin (HY-15142A)-induced cell death in vitro. NecroX-2 can be used for research on neurological diseases.
    NecroX-2
  • HY-179063
    5-HT2A receptor agonist-13 98%
    5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT2A receptor, with an EC50 value of 416.9 nM and a Ki value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the 5-HT2B receptor (EC50 = 120.2 nM), D2 receptor (Ki = 1298 nM), and has no activity towards the 5-HT2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC50 = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD).
    5-HT2A receptor agonist-13
  • HY-179071
    DAPK1 ligand-1 3057532-78-9
    DAPK1 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC DAPK1 Degrader-1 (HY-179055). PROTAC DAPK1 Degrader-1 is a potent LAG-3 PROTAC degrader with neuroprotective activity.
    DAPK1 ligand-1
  • HY-179093
    KCNT1-IN-3 2540501-85-5
    KCNT1-IN-3 (Compound 31) is a KCNT1 inhibitor with an IC50 value of 30 nM against the wild-type human KCNT1. KCNT1-IN-3 can be used in the research of epilepsy.
    KCNT1-IN-3
  • HY-179108
    NMDAR modulator 1
    NMDAR modulator 1 (Compound 12) is a positive, allosteric GluN1/GluN2B receptor modulator. NMDAR modulator 1 enhances NMDAR current. NMDAR modulator 1 can be used in the research of psychiatric disorders.
    NMDAR modulator 1
  • HY-179121
    AChE-IN-97 98%
    AChE-IN-97 (compound 7e) is a cholinesterase inhibitor. AChE-IN-97 exhibits AChE and BChE inhibitory activity through molecular docking. AChE-IN-97 can be used for research on neurological conditions.
    AChE-IN-97
Cat. No. Product Name / Synonyms Application Reactivity