Neurological Disease

MAO-B-IN-7 is a potent and blood-brain barrier permeable MAO-B and AChE inhibitor with IC₅₀s of 41 nM, 87 nM and 0.3 μM for human AChE, electric eel AChE and MAO-B, respectively. MAO-B-IN-7 can effectively alleviate oxidative stress and neuroinflammatory damage.

Rivanicline (RJR-2403) fumarate is a neuronal nicotinic receptor agonist. Rivanicline fumarate is highly selective for the rat brain cortex nAChRs (K_i = 26 nM, EC₅₀ of 732 nM) and α4β2 subtype (K_i = 26 nM, EC₅₀ = 16 μM). Rivanicline fumarate can significantly restore the learning impairment and cognitive dysfunction. Rivanicline fumarate can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).

Isoapoptolidin is a mitochondrial F0F1-ATPase inhibitor (K_i>100 μM, selective for mitochondrial complex V). Isoapoptolidin is promising for research of mitochondrial energy metabolism-related diseases (e.g., cancer, neurodegeneration).

Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity.

NMDA-IN-2 (compound 6b), a Procaine derivative, is a NMDA receptor 2B subtype inhibitor.

TMN-OMe is a blood-brain barrier-permeable GPR39 agonist and a radiotracer for positron emission tomography (PET). TMN-OMe activates GPR39 by recruiting β-arrestin, exhibits highly selective binding ability in the mouse brain, and enables quantitative analysis of GPR39 at the in vivo level. TMN-OMe shows specific uptake in GPR39 knockout mice, Alzheimer's disease model (APP/PS1) mice, and blocking experiments. TMN-OMe facilitates in-depth exploration of changes in GPR39-related mechanisms in neurological diseases and is widely used in Alzheimer's disease research.

Brinzolamide (AL-4862) hydrochloride is a selective carbonic anhydrase II inhibitor with an IC₅₀ value of 3.2 nM. Brinzolamide hydrochloride reduces intraocular pressure (IOP) by inhibiting ciliary CA-II and decreasing atrial fluid secretion. Brinzolamide hydrochloride can be used in glaucoma disease research.

Selnoflast (RO7486967) monopotassium, formerly somalix/RG6418/IZD334 monopotassium, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast monopotassium is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast monopotassium is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease.

Azo-enkephalin is an endorphin analog with significant analgesic activity. Azo-enkephalin can be used in the development of opioid analgesics.

Synephrine (Standard) is the analytical standard of Synephrine. This product is intended for research and analytical applications. Synephrine (Oxedrine), an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine is a sympathomimetic compound and can be used for weight loss.

Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC₅₀ of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate.

FTO-IN-17 is an orally active and brain-penetrant FTO (m₆A RNA demethylase) inhibitor with an IC₅₀ of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m₆A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models.

GSNOR-IN-1, a prodrug of GSNOR-IN-2 (HY-176275), is a BBB-penetrable S-nitrosoglutathione reductase (GSNOR) inhibitor. GSNOR-IN-1 has significant protective activity against OGD/R-induced injury. GSNOR-IN-1 regulates calcium signaling and synaptic function via Clstn1 S-nitrosation and inhibits neuronal apoptosis. GSNOR-IN-1 significantly reduces infarct volume while improving neurological deficits in ischemic stroke rat models. GSNOR-IN-1 has neuroprotective activity, promising for ischemic stroke research.

Olivetol-d₉ is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activities.

AChE-IN-43 is a potent and selective inhibitor of AChE with a K_i of 0.41 μM. AChE-IN-43 can be used in study neurological disease.

SB-414796 is a selective, orally active and cross the blood-brain barrier dopamine D3 receptor antagonist with K_i values of 4, 400 nM for D3, D2, respectively.

ABT-418 is a selective neuronal nicotinic acetylcholine receptor ligand with activity in improving spatial memory. ABT-418 administered before training can significantly reduce the spatial discrimination deficit caused by ventricular damage. ABT-418 is considered to be a potential treatment for attention deficit disorder.

Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain.

[D-Ala2]-Met-Enkephalin, an opioid peptide, is a potent opioid agonist. [D-Ala2]-Met-Enkephalin inhibits ACh-induced and suckling-induced oxytocin (OT) release.

(Rac)-Sabcomeline ((Rac)-SB-202026) serves as an M1/M4 muscarinic agonist, making it a valuable tool in the exploration of neurological disorders, including schizophrenia.