Neurological Disease

RI-OR2-TAT is a brain-penetrant inhibitor of β-Amyloid oligomerization, which is produced by adding the HIV protein transduction domain TAT to RI-OR2. RI-OR2-TAT binds to Aβ42 fibrils with a K_d value of 58-125 nM. RI-OR2-TAT reduces Aβ aggregation and plaque levels, reduces activation of microglia and oxidative damage, and increases the number of young neurons in the dentate gyrus.

Haloperidol-d₄ is deuterium labeled haloperidol, and the latter is a potent dopamine D2 receptor antagonist.

Papaveroline is a Fyn tyrosine kinase inhibitor, Na⁺,K⁺-ATPase inhibitor with an IC₅₀ of 0.20 mM, Mg²⁺-ATPase inhibitor, K⁺-activated pNPPase inhibitor with an IC₅₀ of 1.51 mM, and apoptosis inducer. Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues. Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels. Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease. Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease.

KLH45b is an inhibitor of DDHD2 (DDHD domain containing 2).

Axomadol (EN3324) is a centrally active analgesic agent with opioid agonistic properties and inhibitory effects on the reuptake of monoamines.

Lubeluzole dihydrochloride is the dihydrochloride salt of Lubeluzole (HY-105084). Lubeluzole dihydrochloride is the S-isomer of benzothiazole derivative. Lubeluzole dihydrochloride can inhibit glutamate release, glutamate-activated NO synthesis and block voltage-gated Sodium Channel and Calcium Channel. Lubeluzole dihydrochloride exhibits anti-ischemic and neuroprotective effects. Lubeluzole dihydrochloride also shows anti-bacterial and anti-diarrheal potential. Lubeluzole dihydrochloride can inhibit cardiac sodium channel and prolong cardiac action potential. Lubeluzole dihydrochloride can inhibit cancer cells proliferation and invasion and shows chemosensitizing effect. Lubeluzole dihydrochloride can be used for the researches of cancer, infection, neurological and cardiovascular disease such as stroke, infectious diarrhea and ovarian.

MAO-B-IN-18 is a potent and selective MAO B inhibitor with IC₅₀s of 52 nM and 14 μM for hMAO B and hMAO A, respectively. MAO-B-IN-18 enables promising cytoprotective effects against hydrogen peroxide insults in neuroblastoma and astrocytes cultures.

Methyl 3-O-methylgallate (M3OMG) possesses antioxidant effect and can protect neuronal cells from oxidative damage.

(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum.

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM.

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with K_i values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

Amoxapine (Standard) is the analytical standard of Amoxapine. This product is intended for research and analytical applications. Amoxapine (CL-67772) is a norepinephrine reuptake blocker and a 5-HT₂/5-HT₃ antagonist. Amoxapine can be used for the research of depression. Amoxapine has antibacterial activity. Amoxapine can enhance the killing effect of macrophages on mycobacterium by inducing autophagy, while protecting the cells from death.

GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC₅₀ values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.

ML254 is a potent mGlu₅ potentiator, with EC₅₀ and pEC₅₀ of 9.3 nM and 8.03 nM for rat mGlu₅, respectively. ML254 can be used for researching schizophrenia. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of NET, stabilizing the inward-open state and has a preferential NET/SERT inhibition with pIC₅₀ = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions.

VUF10166 is a potent and high-affinity 5-HT₃ receptor antagonist, with K_i values of 0.04 nM (5-HT₃A) and 22 nM (5-HT₃AB). VUF10166 inhibits 5-HT-induced responses at 5-HT₃A and 5-HT₃AB receptors at nanomolar concentrations. At 5-HT₃ receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC₅₀ of 5.2 μM.

Levetimide is a potent and stereoselective inhibitor of [³H](+)pentazocine binding, with a K_i of 2.2 nM.

Prucalopride-¹³C,d₃ is the ¹³C- and deuterium labeled Prucalopride.

Mevalonic acid (MVA) is a precursor substance of the mevalonate pathway, which is essential for cell growth and proliferation. Mevalonic acid is effective in inhibiting Simvastatin (HY-17502)-induced decrease in C2C12 cell viability in vitro. Mevalonic acid can be used in studies of myopathy and heart failure.

GSK3039294 is an orally active pro-drug of Miridesap (HY-101861), a circulating serum amyloid P component depleter. GSK3039294 undergoes hydrolysis to form miridesap via a monoester intermediate. GSK3039294 can be used for the research of systemic amyloidosis.