Neurological Disease

EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitory activity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy.

(S)-2-Ketodoxapram ((S)-AHR 5955) is a metabolite of Doxapram (HY-B0551). Doxapram is a respiratory stimulant^[1][2].

SCH 60057 (Compound 7) is a neurokinin (NK) receptor inhibitor that can be isolated from Acremonium sp., with IC₅₀ values of 6 μM and 12 μM for NK₁ and NK₂, respectively.

L-Hyoscyamine (sulfate) (Standard) is the analytical standard of L-Hyoscyamine (sulfate). This product is intended for research and analytical applications. L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205).

JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .

L-Aspartic acid-¹⁵N,d₃ is the ¹⁵N, deuterated-labeled L-Aspartic acid (HY-N0666). L-Aspartic acid is a NMDA receptor agonist and acidic amino acid. L-Aspartic acid has no independent analgesic activity. L-Aspartic acid can antagonize the analgesic effects of D-Aspartic acid and Morphine. L-Aspartic acid regulates polymorph transformation, crystal growth/aggregation and nucleation processes of calcium carbonate, and can serve as a biomineralization template. L-Aspartic acid promotes burst firing of central neurons. L-Aspartic acid can be used in studies related to cerebral ischemia and epilepsy.

MAO-B-IN-56 is a multi-target-directed ligand with AChE, BChE, MAO-B, and BACE1 inhibitory activity, with IC₅₀ values of 0.35 μM, 3.22 μM, 0.14 μM, and 3.85 μM respectively, and shows selectivity for AChE over BChE and MAO-B over MAO-A.MAO-B-IN-56 reduces amyloid-beta production, reduces paw edema, improves spatial memory, and enhances Alzheimer's disease hallmarks and associated histopathological alterations.MAO-B-IN-56 can be used for the research of alzheimer's disease.

Ebiratide (HOE-427 free base) is an ACTH 4-9 derivative, which acts directly on the central nervous system and exhibits memory-enhancing efficacy. Ebiratide enhances acetycholine (ACh) metabolism in rat brain.

Agouti-Related Protein (25-51) (human) (AGRP (25-51) (human)) is an amino-terminal 25-51 fragment of agouti-related protein (AGRP).

Pep1-TGL is a synthetic peptide containing the TGL motif from the C-terminus of the AMPA receptor GluA1 subunit.

M1 mAChR modulator-1 (Example 66) is a muscarinic M1 receptor (mAChR1) positive allosteric modulator. M1 mAChR modulator-1 effectively promotes gastrointestinal motility and defecation in mouse models with low central permeability. M1 mAChR modulator-1 can be used for constipation research.

TOP1362 is a narrow spectrum kinase inhibitor. TOP1362 is a potent inhibitor of P38-α and Syk kinases with K_d values of 26 and 18 nM, respectively and an IC₅₀ of 14 nM in the Src kinase activity assay. TOP1362 potently inhibits P38-α, Src and Syk. TOP1362 can be used in the research of dry eye syndrome.

4-Chlorokynurenine (4-Cl-KYN) is a prodrug of 7-Chlorokynurenic acid (NMDA receptor antagonist) (HY-100811). 4-Chlorokynurenine has orally activity and blood-brain permeability. 4-Chlorokynurenine can reduce depressive symptoms and neurotoxicity. 4-Chlorokynurenine can be used for the research of neurological disease, such as depression and seizure.

5-HT2C agonist-4 (Compound 3i) is an agonist for 5-HT2C receptor with an EC₅₀ of 5.7 nM. 5-HT2C agonist-4 reduces locomotor activity in the zebrafish larval model.

COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC₅₀ of 0.12 μM against HDAC6 and an IC₅₀ of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease.

Bovine calmodulin can be used for the in vitro phosphorylation assay of recombinant retinoic acid-induced gene I protein. Bovine calmodulin has also been used in studies of the hydrolysis and deamidation of the endopeptide Glu-C protein.

LSD1-IN-49 hydrochloride (Compound (±) 1) is an irreversible LSD1/KDM1A inhibitor with an IC₅₀ of 29 nM against hLSD1. LSD1-IN-49 hydrochloride irreversibly inhibits the enzymatic activity of LSD1 by forming an adduct with flavin adenine dinucleotide (FAD) in the binding pocket of LSD1. LSD1-IN-49 hydrochloride is applicable to research related to schizophrenia, autism spectrum disorder and Huntington's disease.

D-Cysteine (Standard) is the analytical standard of D-Cysteine. This product is intended for research and analytical applications. D-Cysteine, the D-isomer of cysteine, is an orally active antibacterial agent and a regulator of neural progenitor cell proliferation. D-Cysteine can inhibit Escherichia coli, Streptococcus mutans, and Streptococcus sanguinis. The no-observed-adverse-effect level of D-Cysteine in rats should be less than 500 mg/kg/day[1][2][3][4].

AChE/BChE/MAO-B-IN-1 is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC₅₀ values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity.

Lignoceric acid (Standard) is the analytical standard of Lignoceric acid. This product is intended for research and analytical applications. Lignoceric acid (Tetracosanoic acid) is a 24-carbon saturated (24:0) fatty acid, which is synthesized in the developing brain. Lignoceric acid is also a by-product of lignin production. Lignoceric acid can be used for Zellweger cerebro‐hepato‐renal syndrome and adrenoleukodystrophy research[1][2].