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.

Art. -Nr. Produktname CAS. Nr. Reinheit Chemische Struktur
  • HY-12355S
    Siponimod-d11 2104759-32-0 98%
    Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis.
    Siponimod-d11
  • HY-123567
    LY86057 148966-66-9 98%
    LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
    LY86057
  • HY-123594
    R-2 Methanandamide 157182-47-3 98%
    R-2 Methanandamide (Compound 2) is a cannabinoid Anandamide (HY-10863) analog with a Ki of 119 nM for the cannabinoid receptor (Ki is determined using rat brain membranes with PMSF).
    R-2 Methanandamide
  • HY-123612
    JAS239 98%
    JAS239 is a blood-brain barrier-permeable ChoK inhibitor. JAS239 inhibits phosphocholine synthesis and reduces the expression level of E2F1 protein. JAS239 exhibits near-infrared fluorescence properties. JAS239 exerts anti-tumor activity against glioblastoma. JAS239 can be used in studies related to glioblastoma.
    JAS239
  • HY-123654
    L-796449 194608-80-5 98%
    L-796449 is a potent PPARγ agonist. L-796449 shows neuroprotective. L-796449 has the potential for the research of stroke.
    L-796449
  • HY-123655
    Fenazinel dihydrochloride 685138-02-7 98%
    Fenazinel dihydrochloride, an N-methyl-D-aspartate (NMDA) receptor antagonist, shows promise as a potential treatment for ischemic stroke.
    Fenazinel dihydrochloride
  • HY-123661
    MIPS1455 1627580-82-8 98%
    MIPS1455 is a light-activated M1 muscarinic acetylcholine receptor ligand with irreversible binding activity to the allosteric site of the receptor. MIPS1455 is a drug target under investigation for the suppression of cognitive deficits and may become a valuable molecular tool for further investigation of allosteric interactions of the receptor.
    MIPS1455
  • HY-123665
    PSB-1410 1494477-03-0 99.22%
    PSB-1410 is a monoamine oxidase B (MAO-B) inhibitor, with an IC50 of 0.227 nM against human MAO-B and an IC50 of 1.01 nM against rat MAO-B. PSB-1410 can be used for the research of Parkinson's disease.
    PSB-1410
  • HY-123677
    E2508 685886-34-4 98%
    E2508 is an orally active corticotropin-releasing factor 1 (CRF1) receptor antagonist with a Ki value of 11 nM for hCRF1.
    E2508
  • HY-123681
    R 57720 98164-11-5 98%
    R 57720 is an antiepileptic agent that exhibits dose-dependent anticonvulsant activity across multiple postnatal rat age groups. R 57720 inhibits severe generalized tonic-clonic seizures induced by Pentylenetetrazol. R 57720 can be used for epilepsy research.
    R 57720
  • HY-123704
    CGS-12066 maleate 1350965-83-1 98%
    CGS-12066 (maleate) is a 5-HT receptor agonist. CGS-12066 has agonist effect for 5-HT1A , 5-HT1B ,5-HT1C and 5-HT1D with pEC50 values of 6.41, 7.56, 4.05 and 7.11, respectively. CGS-12066 can be used for the research of neurological disease.
    CGS-12066 maleate
  • HY-123743
    JNJ-42314415 1334165-90-0 98%
    JNJ-42314415 is a centrally active phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 35 nM and 64 nM for human recombinant PDE10A and rPDE10A, respectively.
    JNJ-42314415
  • HY-123745
    Aβ aggregation-IN-6 439932-74-8 98%
    Aβ aggregation-IN-6 is an Aβ aggregation inhibitor with ~60-70% inhibition of Aβ17-40 aggregation. Aβ aggregation-IN-6 stabilizes Aβ dimer assembly, binds to Aβ steric-zipper assembly. Aβ aggregation-IN-6 can be used for the research of alzheimer's disease.
    Aβ aggregation-IN-6
  • HY-123778
    VU6007678 2222737-15-5 98%
    VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke.
    VU6007678
  • HY-123807
    JNJ-5234801 426227-09-0 98%
    JNJ-5234801 is an orally active anxiolytic that targets the 5-HT2 receptor. JNJ-5234801 increases water intake and reduces alcohol preference in rats. JNJ-5234801 could be used in studies on anxiety and alcoholism.
    JNJ-5234801
  • HY-123836
    MK-7288 936626-07-2 98%
    MK-7288 is a histamine H3 receptor inverse agonist. MK-7288 can prolong sleep latency in the Maintain Wake Test (MWT). MK-7288 can be used in research on obstructive sleep apnea (OSA) and excessive daytime sleepiness (EDS).
    MK-7288
  • HY-12383S
    Pelubiprofen-13C,d3 98%
    Pelubiprofen-13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
    Pelubiprofen-13C,d3
  • HY-123852
    PF-06764427 1842371-08-7 98%
    PF-06764427 is a selective M1 muscarinic acetylcholine receptor positive allosteric modulator. PF-06764427 exhibits robust M1 agonist activity. PF-06764427 can be used in the research of Alzheimer's disease and schizophrenia.
    PF-06764427
  • HY-123858
    VU6001221 2002495-17-0 98%
    VU6001221 is a blood-brain barrier permeable Choline Transporter (CHT) inhibitor (IC50 = 270 nM). VU6001221 increases the likelihood of extracellular choline elevation activating synaptic α7 nicotine ACh receptors. VU6001221 attenuates potassium-induced ACh levels in the prefrontal cortex.
    VU6001221
  • HY-123859
    SR-2890 1454584-91-8 98%
    SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values ​​of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease.
    SR-2890
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