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-173024
    TRPC4/5-IN-3 3053390-98-7 98%
    TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87%.
    TRPC4/5-IN-3
  • HY-173025
    Nurr1 agonist 12 98%
    Nurr1 agonist 12 (Compound 37) is the agonist for nuclear receptor-associated protein 1 (Nurr1) that activates the transcriptional activity of Nurr1 with an EC50 of 0.06 μM. Nurr1 agonist 12 activates the human response elements NBRE, NurRE, and DR5 with EC50 of 0.07 μM, 0.027 μM, and 0.014 μM, respectively. Nurr1 agonist 12 induces the expression of Nurr1-regulated neurotrophic genes, such as tyrosine hydroxylase (TH), SOD1/2, BDNF, Sestrin 3, and BIRC5 (Survivin). Nurr1 agonist 12 exhibits neuroprotective efficacy against Paraquat-induced neurotoxicity.
    Nurr1 agonist 12
  • HY-173030
    Opioid receptor agonist 1 98%
    Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with Ki of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models.
    Opioid receptor agonist 1
  • HY-173031
    KTX-005 162182-77-6 98%
    KTX-005 is the agonist for mAChR that regulates the signaling pathway of the neurotransmitter acetylcholine, and can be used for research of schizophrenia.
    KTX-005
  • HY-173032
    VU6033685 98%
    VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%.
    VU6033685
  • HY-173044
    5-HT1AR/5-HT6R ligand-1 98%
    5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM.
    5-HT1AR/5-HT6R ligand-1
  • HY-173046
    NLRP3-IN-71 3026419-44-0 98%
    NLRP3-IN-71 (Compound 19) is a BBB-permeable, orally active and selective NLRP3 inhibitor that can inhibit IL-1β secretion. NLRP3-IN-71 can be used for the research of neurodegenerative diseases.
    NLRP3-IN-71
  • HY-173049
    2N4R Tau/α-Syn against-1 98%
    2N4R Tau/α-Syn against-1 (Compound 4d) targets α-synuclein and tau protein, inhibits the fibrillation and oligomer formation of α-synuclein and tau proteins, exhibits disaggregation activity on Aβ fibers. 2N4R Tau/α-Syn against-1 can be used in research of Parkinson's disease and Alzheimer's disease.
    2N4R Tau/α-Syn against-1
  • HY-173083
    MDA7 1103840-28-3 98%
    MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models.
    MDA7
  • HY-173138
    FCOB02 3064236-41-2 98%
    FCOB02 is a monoamine oxidase B (MAO-B) ligand. FCOB02 can be labeled as [18F]FCOB02, a 4-methylcoumarin-like targeting probe. [18F]FCOB02 has a high affinity for MAO-B with an IC50 of 10.68 nM. [18F]FCOB02 can be used in specific MAO-B imaging as well as quantitative analysis in vivo.
    FCOB02
  • HY-173142
    Neuroprotective agent 7 98%
    Neuroprotective agent 7 (Compound 13) is a BBB-penetrable neuroprotective agent. Neuroprotective agent 7 has a powerful neuroprotective effect and can reduce the cerebral infarct area in the MCAO rat model. Neuroprotective agent 7 can be used in the research of diseases such as cerebral ischemia.
    Neuroprotective agent 7
  • HY-173144
    AChE-IN-85 98%
    AChE-IN-85 (Compound 7k) is an AChE inhibitor with an IC50 of 0.083 μM. AChE-IN-85 can inhibit the release of NO, the production of TNF-α and IL-1β, the levels of LDH and ROS, as well as the aggregation of Aβ42. AChE-IN-85 has anti-inflammatory and neuroprotective effects and can be used in the research of diseases such as Alzheimer's disease.
    AChE-IN-85
  • HY-173152
    AChE/BChE-IN-26 98%
    AChE/BChE-IN-26 (Compound 20aa) is a cholinesterase inhibitor with IC50 values of 0.75 μM and 4.11 μM against eeAChE and eqBChE, respectively. AChE/BChE-IN-26 has antioxidant activity and can be used in the research of diseases such as Alzheimer's disease.
    AChE/BChE-IN-26
  • HY-173156
    UNC10013 98%
    UNC10013 is a SETDB1 allosteric modulator that forms a covalent bond with Cys385 in the 3TD domain, exhibiting negative allosteric regulatory activity. It has a kinact/KI value of 1.0 × 106 M-1*s-1. UNC10013 effectively disrupts SETDB1-mediated Akt methylation and holds potential value for research in cancer and neurodegenerative diseases.
    UNC10013
  • HY-173181
    Anticonvulsant agent 10 98%
    Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a potent ED50 of 0.04 mmol/kg. By inhibiting Keap1-Nrf2 binding and activating the Nrf2/ARE pathway, Anticonvulsant agent 10 exerts anticonvulsant and neuroprotective effects, making it suitable for research in antiepileptic and neuroprotective studies.
    Anticonvulsant agent 10
  • HY-173221
    MJ210 98%
    MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone (HY-B1756) to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease.
    MJ210
  • HY-173226
    BACE1-IN-15 98%
    BACE1-IN-15 (Compound 72) is a selective inhibitor of beta-site amyloid precursor protein cleaving enzyme 1 (BACE-1) with oral activity and the ability to penetrate the blood-brain barrier. Its IC50 value is 121.65 nM (the IC50 value for BACE-2 is 480.92 nM). BACE1-IN-15 can be used in the research of the Alzheimer's disease field
    BACE1-IN-15
  • HY-173263
    AChE-IN-86 98%
    AChE-IN-86 (Compound 6f) is an inhibitor of enzyme acetylcholinesterase (AChE) with IC50 values of 25.33 μg/mL. AChE-IN-86 exerts inhibitory activity against AChE through forming hydrogen bonds, π-π and π-alkyl interactions with amino acid residues at the key catalytic sites of AChE. AChE-IN-86 can be used for Alzheimer's disease study.
    AChE-IN-86
  • HY-173276
    SARM1-IN-4 3069378-18-0 98%
    SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor. After being orally administered at a dose of 50 mg/kg in a mouse model, it can reduce the level of plasma neurofilament light chain (NfL). SARM1-IN-4 prevents programmed axonal degeneration by inhibiting the NAD+ hydrolase activity of SARM1, and it can be used in research related to neurodegenerative diseases and neurological disorders (such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathies, etc.).
    SARM1-IN-4
  • HY-173282
    Aβ aggregation-IN-2 98%
    Aβ aggregation-IN-2 (Compound 8i) is an inhibitor of amyloid-β protein (Aβ42) aggregation, showing approximately 91% inhibition of Aβ42 aggregation at 25 μM. It also exhibits Aβ42 disaggregation effects and antioxidant activity. Aβ aggregation-IN-2 can be used for research in the field of Alzheimer's disease.
    Aβ aggregation-IN-2
Cat. No. Product Name / Synonyms Application Reactivity