Neurological Disease

Tetrabenazine-d₇ (TBZ-d₇-d₇) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 K_i 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.

Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D₂ receptor biased agonism ligand with an K_i value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis.

BB-22 is a cannabinoid wih dopamine (DA) stimulant properties. BB-22 shows affinity to CB1 receptors with a K_i value of 0.11 nM and an EC₅₀ value of 2.9 nM.

18α-Glycyrrhetinic acid (Standard) is the analytical standard of 18α-Glycyrrhetinic acid. This product is intended for research and analytical applications. 18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis.

rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M₂-adrenoceptor antagonist and α₂-adrenoceptor antagonist. rel-Delequamine has a pK_i of 9.45 for α₂-adrenoceptors in the rat cortex. rel-Delequamine augments K⁺-evoked release of noradrenaline with an EC₅₀ of 1 nM.

Carbonic anhydrase inhibitor 17 (compound 7c) ,pyridazine-tethered sulfonamide, is a carbonic anhydrase II inhibitor with IC₅₀ of 0.63 nM.

Ipenoxazone (MLV-6976) hydrochloride is a potent and centrally acting muscle relaxant.

Lurasidone Metabolite 14283-d₈ is the deuterium labeled Lurasidone Metabolite 14283, which is a metabolite of Lurasidone.

5-HT1AR agonist 3 (Compound 77) is a 5-HT1A agonist. 5-HT1AR agonist 3 has 5-HT1A receptor agonist activity (EC₅₀: 1.3 nM). 5-HT1AR agonist 3 mainly exerts its effects by activating 5-HT1A receptors and can be used in the study of neuropsychiatric diseases such as anxiety, depression and sleep disorders.

HV1-IN-1 hydrochloride is an inhibitor of the human voltage-gated proton channel (hHV1). HV1-IN-1 hydrochloride works by binding to the VSD of the HV1 channel. The VSD is a component of the HV1 channel that is responsible for detecting changes in membrane potential and triggering the opening of the channel. HV1-IN-1 hydrochloride can be used in the study of cancer, neuroinflammation and immune response.

NW-1689 is a process-related impurity of safinamide mesilate (SAFM). SAFM can be used for the study of Parkinson's disease (PD). It is a highly selective and reversible inhibitor of monoamine oxidase-B (MAO-B) and also blocks sodium channels and N-type calcium channels. These effects of SAFM help reduce the breakdown of dopamine and inhibit the release of glutamate. NW-1689 has a similar chemical structure to SAFM and has some similar pharmacological effects as SAFM, and can be used in Parkinson's disease research.

Org 12962 hydrochloride is a potent, selective and efficacious 5-HT_2C receptor agonist and exhibits pEC₅₀ values of 7.01, 6.38 and 6.28 for 5-HT_2C, 5-HT_2A and 5-HT_2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.

Neostigmine iodide is a reversible acetylcholinesterase inhibitor with muscle tone-enhancing activity. Neostigmine iodide is primarily used to improve muscle function in patients with myasthenia gravis. Neostigmine iodide is also used in routine anesthesia to reverse the effects of nondepolarizing muscle relaxants such as rocuronium.

5-LOX/MAOs-IN-1 (compound 3) is a 5-LOX/MAOs inhibitor and a potent free radical scavenger with antioxidant properties. 5-LOX/MAOs-IN-1 also showed neuroprotective activity in oxidative stress-damaged cell models and can activate the neurogenesis microenvironment of adult mouse neural stem cells. 5-LOX/MAOs-IN-1 can be used for the study of neurodegenerative diseases.

AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC₅₀ values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research.

L-663581 (FG-8205) is an agonist of benzodiazepine receptor, acting as a partial agonist at GABA A receptor.

HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC₅₀ of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H₂O₂-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability.

DSPE-PEG2000-Maleimide free acid is a phospholipid-PEG conjugate. DSPE-PEG2000-Maleimide free acid utilizes the amphiphilicity of DSPE to insert into the lipid bilayer of liposomes or nanoparticles. DSPE-PEG2000-Maleimide free acid covalently couples to the sulfhydryl (-SH) of ligands (such as antibodies, peptides, or proteins) via thiol-maleimide click chemistry, giving the particles targeting capabilities. DSPE-PEG2000-Maleimide free acid can be used in the researches of breast cancer, lymphoma, and inherited retinal degeneration.

MAP4343-d₄ is the deuterium labeled MAP4343. MAP4343 is the 3-methylether derivative of Pregnenolone. MAP4343 binds in vitro to microtubule-associated protein 2 (MAP2), stimulates the polymerization of tubulin, enhances the extension of neurites and protects neurons against neurotoxic agents.

Chlorbenside (Standard) is the analytical standard of Chlorbenside. This product is intended for research and analytical applications. Chlorbenside is an organochlorine pesticide. Chlorbenside targets organism such as mites and ticks and possesses efficient ovicidal and larvicidal activities.