2. Neurological Disease

Neurological Disease

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-161273
    TRPV1 antagonist 6
    TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration.
    TRPV1 antagonist 6
  • HY-161282
    hCAII-IN-10
    hCAII-IN-10 (compound 11d) is hCA II inhibitor with the IC50s of 14 nM and 29.2 μM for hCA II and hCA I, respectively. hCAII-IN-10 inhibits cell growth against HT-29 cells with the IC50 of 74 μM. hCAII-IN-10 shows strongly lowered intraocular pressure in the glaucomatous rabbit eye model.
    hCAII-IN-10
  • HY-161311
    AChE/BChE-IN-18
    AChE/BChE-IN-18 (Compound 4g) is a dual inhibitor of AChE/BChE , with a IC50 value of 0.315 μM for AchE. AChE/BChE-IN-18 is also a CB2R antagonist with a Ki value of 31 nM. AChE/BChE-IN-18 has neuroprotective activity.
    AChE/BChE-IN-18
  • HY-161316
    NNMT-IN-5
    NNMT-IN-5 (Compound 3-12) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 47.9 ± 0.6 nM). NNMT-IN-5 also has an excellent selectivity profile over a panel of human methyltransferases. NNMT-IN-5 can be used for the research of cancer, diabetes, metabolic disorders, and neurodegenerative diseases.
    NNMT-IN-5
  • HY-161328
    MAO-B-IN-31
    MAO-B-IN-31 (Compound 30) is an effective and selective inhibitor of monoamine oxidase B (monoamine oxidase B). The IC50 value is 41 nM. MAO-B-IN-31 also inhibits α-syn and tau aggregation. MAO-B-IN-31 has neuroprotective activity.
    MAO-B-IN-31
  • HY-161331
    S16–1029 2653349-51-8
    S16–1029 is a selective and orally active butyrylcholinesterase (BChE) inhibitor with IC50s of 11.35 nM and 48.1 nM for eqBChE and hBChE, respectively. S16–1029 could cross the blood-brain barrier (BBB) and reach the central nervous system (CNS). S16–1029 can be used for Alzheimer's disease (AD) research.
    S16–1029
  • HY-161359
    BACE1-IN-14
    BACE1-IN-14 (compound 27f) is a BACE1 inhibitor, with the EC50 values of 0.7 μM and 1.6 μM for BACE1 and BACE2. BACE1-IN-14 is can be used in Alzheimer's disease (AD) research.
    BACE1-IN-14
  • HY-161405
    NPFF1-R antagonist 1 3057753-40-6
    NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.
    NPFF1-R antagonist 1
  • HY-161418
    1-NBX
    1-NBX is a potent and selective A1R ligand. 1-NBX exhibits significantly improved A1R affinity with with a Ki of 2.6 nM and lower affinity for the A2A receptor with a Ki of 164 nM.
    1-NBX
  • HY-161420
    TRPV1 antagonist 7
    TRPV1 antagonist 7 (Compound 36) is a selective TRPV1 antagonist that effectively blocks capsaicin activation (IC50=2.31 nM). TRPV1 antagonist 7 can be used in analgesic research.
    TRPV1 antagonist 7
  • HY-161433
    VMAT2-IN-3
    VMAT2-IN-3 (compound 10) is a potent vesicular monoamine transporter-2 (VMAT2) inhibitor with a Ki of 0.71 nM. VMAT2-IN-3 has the potential for neurological or psychiatric disease research.
    VMAT2-IN-3
  • HY-161448
    Tau-aggregation-IN-3 3032869-59-0
    Tau-aggregation-IN-3 (compound 9) a Tau protein aggregation inhibitor (TAI). Tau-aggregation-IN-3 shows activity in cell-based aggregation inhibition experiments (EC50=4.816 μM). Tau-aggregation-IN-3 can be used in Alzheimer's disease research.
    Tau-aggregation-IN-3
  • HY-161453
    BChE-IN-32
    ChE-IN-32 (compound 5d) is a potent and selective hBChE inhibitor with an IC50 value of 0.109 µM. BChE-IN-32 shows cytotoxicity. BChE-IN-32 has the potential for the research of Alzheimer's disease.
    BChE-IN-32
  • HY-161458
    GSK-3β inhibitor 16
    GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC50 of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice.
    GSK-3β inhibitor 16
  • HY-161461
    E234G HYPE-IN-1 1341007-95-1
    E234G HYPE-IN-1 (Compound I2.10) is an inhibitor of AMPylation directed by the Huntingtin-interacting protein E (HYPE), possessing low micromolar bioactivity, low cytotoxicity, and blood-brain barrier permeability. E234G HYPE-IN-1 can inhibit the AMPylation of B-cell immunoglobulin-binding protein (BiP), the primary substrate of HYPE. E234G HYPE-IN-1 is suitable for development as a HYPE-specific therapeutic agent for clinical conditions such as neurodegenerative diseases and diabetes.
    E234G HYPE-IN-1
  • HY-161466
    AChE-IN-62
    AChE-IN-62 (Compound 1) is an effective mixed and selective acetylcholinesterase (AChE) inhibitor with an IC50 value of 0.421 μM. AChE-IN-62 exhibits excellent blood-brain barrier permeability and neuroprotective effects. Additionally, AChE-IN-62 can inhibit the aggregation of Aβ1-42 with an IC50 value of 44.64 μM. AChE-IN-62 is also an effective multi-target-directed ligand (MTDL) that can be utilized in the research of Alzheimer's disease.
    AChE-IN-62
  • HY-161483
    CBP/p300 ligand 3 1936425-34-1
    CBP/p300 ligand 3 is a target protein ligand of CBPD-268 (HY-161369). CBP and p300 are two proteins with histone acetyltransferase (HAT) activity, and CBP and p300 play key roles in regulating biological processes such as gene expression, cell proliferation, differentiation and DNA repair. Through its acetyltransferase activity, CBP/p300 can acetylate histones and other proteins, thereby regulating chromatin structure and gene expression. CBP/p300 ligand 3 regulates the function of CBP/p300 by binding to a specific domain of the CBP/p300 protein (the bromine domain or HAT domain), inhibiting its enzyme activity or altering its interactions with other proteins (transcription factors). CBP/p300 ligand 3 can be used in cancer, neurodegenerative diseases and other disease models associated with abnormal CBP/p300 function.
    CBP/p300 ligand 3
  • HY-161508
    AChE/BChE-IN-19 3036136-22-5
    AChE/BChE-IN-19 (Compound 12) is a nicotinic hydrazide derivative. AChE/BChE-IN-19 is a inhibitor of AChE (IC50 = 21.45 nM) and BChE (IC50 =18.42 nM). AChE/BChE-IN-19 can be used in Alzheimer's disease research.
    AChE/BChE-IN-19
  • HY-161511
    LPH-5 2641630-97-7
    LPH-5 is a selective 5-HT2A receptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2A receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2A receptor. LPH-5 can be used to further explore the 5-HT2A receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders.
    LPH-5
  • HY-161512
    hAChE/hBACE-1-IN-4 229476-71-5
    hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research.
    hAChE/hBACE-1-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
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