Neurological Disease

Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.

Domperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.

Lixumistat (IM156 free base) is a potent and orally active AMPK activator and OXPHOS inhibitor. Lixumistat strongly activates AMPK, while it lacks the systemic metabolic regulatory effects of classic metformin, such as hypoglycemic and weight-lowering activities. Lixumistat exhibits significant therapeutic effects on cognitive decline associated with brain aging and pulmonary fibrosis.

Pergolide (LY127809 free base), an Ergoline derivative, is a potent and orally active dopamine D₁ and D₂ receptor agonist. Pergolide can be used for Parkinson's disease and hyperprolactinaemia research.

(±)-1,2-Propanediol-d₈ is the deuterium labeled (±)-1,2-Propanediol. (±)-1,2-Propanediol (1,2-(RS)-Propanediol) is an aliphatic alcohol and frequently used as an excipient in many agent formulations to increase the solubility and stability of agents.

AK 295 (CX 295) is a selective calpain inhibitor. AK 295 can inhibit apoptosis through a calpain-dependent pathway. AK 295 shows potent neuroprotective effect. AK 295 can inhibit the activity of the cysteine protease calpain and reduce myocardial injury. AK 295 can be used for the researches of infection, inflammation, cardiovascular and neurological disease, such as stroke and viral myocarditis.

NGP555 is a γ-secretase modulator. NGP555 Lowers the Amyloid Biomarker Aβ42.

AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

MK-7337 is an α-synuclein ligand with an affinity of < 1 nM. MK-7337 labeled with ¹¹C can be used as a PET tracer for neurodegenerative disorders like Parkinson’s disease imagination.

PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

EPI-589, a quinone derivative, is a safe and well tolerated oxidoreductase enzyme inhibitor and a free radical scavenger, with blood-brain barrier permeable and orally available. EPI-589 is a redox-active neuroprotectant that effectively delays the symptoms of motor neuron disease in wobbler mice. EPI-589 can be used in amyotrophic lateral sclerosis (ALS) research.

Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC₅₀ values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder.

HN37 as a potent and chemically stable antiepileptic agent candidate, with an EC₅₀ of 37 nM for KCNQ2. HN37 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Martinostat hydrochloride is a HDAC inhibitor and can be labeled with radionuclides for quantitative imaging of HDACs in vivo in the central nervous system and major peripheral organs.

BPN-15477 is an orally active, blood-brain barrier-permeable splicing modulator compound (SMC). BPN-15477 restores the correct splicing of exon 20 of the elongator complex protein 1 (ELP1) (EC₅₀ = 1.9 μM), thereby significantly increasing the in vivo functional protein levels in all tissues including the brain. BPN-15477 can be used in the research of familial dysautonomia, such as frontotemporal dementia.

Evenamide (NW-3509) is an orally available voltage-gated sodium channel (VGSC) blocker (K_i=0.4 µM) for the research of schizophrenia. Evenamide shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.

SJFα is a selective p38α PROTAC degrader with a DC₅₀ of 7.16   nM and D_max of 97.4%. SJFα is far less effective at degrading p38δ (DC₅₀ = 299 nM). SJFαcan be used for the research of cancer, such as breast cancer.

NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC₅₀ of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.

9-cis-Retinoic acid-d₅ is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

Kainic acid hydrate is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid hydrate induces seizures.