Neurological Disease

GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABA_AR negative allosteric modulator (NAM) with a K_i of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety.

NUAK1-IN-1 (Compound 9) is a NUAK1 (IC₅₀ of 5.012 nM) and CDK4 inhibitor. NUAK1-IN-1 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.

BNC-1 is an Elk-1 activator that can promote phosphorylation and activation of Elk-1.

BTG 1640 (ABIO-08/01) is a potent anxiolytic isoxazoline. BTG 1640 is a selective inhibitor of GABA- and glutamate-gated chloride channels.

P2X7 receptor antagonist-6 (Compound 2g) is a negative allosteric P2X7 receptor antagonist with an IC₅₀ of 1.31  μM for hP2X7. P2X7 receptor antagonist-6 can be used for cancer, neurodegenerative, inflammatory, and infectious diseases research.

Bromperidol-d₄-1 is deuterium labeled Bromperidol.

Desmethylnortriptyline (Standard) is the analytical standard of Desmethylnortriptyline (HY-100651). This product is intended for research and analytical applications. Desmethylnortriptyline is a metabolite of Amitriptyline (HY-B0527) and Nortriptyline (HY-118620). Desmethylnortriptylineinhibits serotonin and noradrenaline uptake, antagonizes acetylcholine-induced contraction. Desmethylnortriptyline can be used for the research of depression.

DOR agonist 2 (Compound 3) is a Delta Opioid Receptor agonist. DOR agonist 2 can inhibit the expression of TNF-α, prevent NF-κB transport to the nucleus, and activate the G protein-mediated ERK1/2 pathway. DOR agonist 2 can be used in the study of neurodegenerative diseases.

[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system.

KOR agonist 7 (Compound 29) is a highly selective κ-opioid receptor (KOR) agonist with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation.

(-)-Norfenfluramine (l-Norfenfluramine) is a Fenfluramine metabolite. (-)-Norfenfluramine effectively counteracts the zebrafish abnormal locomotor activity. (-)-Norfenfluramine can be used in epilepsy research.

Alkyne-PEG2000-RVG29 is a functionalized PEGylated lipid conjugate composed of three modular components: alkyne (propargyl/alkyne linker) as the lipid anchoring group, a polyethylene glycol (PEG) spacer arm with a molecular weight of 2000 Da, and RVG29 peptide (YTIWMPENPRPGTPCDIFTNSRGKRASNG) (HY-P5623) as the terminal targeting/functional ligand. Alkyne-PEG2000-RVG29 does not contain a lipid anchoring group but instead provides a terminal reactive site for post-assembly ligand or probe conjugation on PEGylated nanoparticles.

Tiquizium bromide is an orally active, atropine-type, nonselective muscarinic antagonist and novel spasmolytic agent. Tiquizium bromide inhibits the developments of gastric lesions and duodenal lesions. Tiquizium bromide induces the mydoriasis and inhibits the Pilocarpine (HY-B0726A)-induced salivation.

PAD3-IN-1 (compound 14b) is an inhibitor of protein arginine deiminase (PAD) and is more than 10-fold more selective for PAD3 than PAD 1, 2, and 4. The IC₅₀ values ​​of PAD3-IN-1 for PAD 1, 2, 3, and 4 are 120, 27.5, 4.5, and 30.5 μM, respectively. And PAD3 is a PAD isoform associated with neurodegenerative responses to spinal cord injury, and PAD3-IN-1 could be used to study PAD-related neurological diseases.

MR-16728 hydrochloride is a compound that promotes the release of acetylcholine and has activity that enhances the release of acetylcholine. MR-16728 hydrochloride inhibits acetylcholine release induced by KCl depolarization. MR-16728 hydrochloride also inhibits Ca(2+)-ATPase activity in pure presynaptic membranes. The half-maximal effect of MR-16728 hydrochloride occurs at a concentration of 13.5 μM. MR-16728 hydrochloride significantly enhances the release of acetylcholine in the presence of low concentrations of calcium (approximately 10 μM range). Enhanced acetylcholine release was also observed with MR-16728 hydrochloride in proteoliposomes loaded with mediator proteins.

Cav 3.2 inhibitor 1 is a T-type calcium channel inhibitor with little binding affinity to dopamine D2 receptors. Cav 3.2 inhibitor 1 can be used for the research of somatic and visceral pain.

TGN, Cys modified is a cysteine modified TGN (HY-P11284) on the C-terminus. TGN, a 12-amino acid ligand, is a BBB-penetrating peptide. TGN can be used as a drug delivery vehicle for Alzheimer's disease research.

Diallyl tetrasulfide is an orally active diallyl tetrasulfide. Diallyl tetrasulfide ameliorates cadmium-induced changes in acetylcholinesterase and adenosine triphosphatase activities as well as oxidative stress injury in the brain of rats. Diallyl tetrasulfide inhibits lipid peroxidation in rat liver microsomes. Diallyl tetrasulfide ameliorates cadmium-induced oxidative liver injury in rats. Diallyl tetrasulfide protects cells against cadmium-induced loss of cell viability, reduces apoptosis rate and ROS production. Diallyl tetrasulfide is applicable to research related to cadmium-induced neurotoxicity and cadmium-induced oxidative liver injury.

CKS peptide is a selective substrate peptide for CK1. CKS peptide can used to measure CK1 activity.

AChE-IN-114 is a selective AChE inhibitor and shows weak inhibitory activity for BChE. AChE-IN-114 can be used for the research of alzheimer’s disease.