Neurological Disease

Syringetin-3-O-glucosid (Syringetin 3-O-β-D-glucoside), a flavonol glycoside, shows relatively weak DPPH and ABTS radical scavenging activity.

Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [³H]histamine release. Thioperamide maleate inhibits [³H]histamine synthesis with a K_i of 31 nM.

Iprindole, an opioid receptor agonist, is a tricyclic antidepressant. Iprindole shortens the immobility time in mice forced swimming test, which can be reversed by the opiate antagonist Naloxone (HY-17417A). Iprindole induces lamellar body formation but devoid of lamellar bodies. Iprindole can be used for the research of depression.

Hydroxytyrosol acetate is an orally active, blood-brain barrier-permeable multi-active compound with multiple effects including antibacterial, antioxidant, anti-platelet aggregation, and neuroprotective activities. Hydroxytyrosol acetate not only inhibits the growth of Vibrio by increasing bacterial membrane permeability, but also interacts with DNA and mediates supercoiled DNA relaxation. Meanwhile, Hydroxytyrosol acetate effectively reduces thrombosis and inhibits lipid oxidation by inhibiting COX activity and promoting vascular nitric oxide production. In terms of neuroprotection, Hydroxytyrosol acetate significantly alleviates neuronal apoptosis and inflammatory responses by up-regulating the expression level of ERβ, thereby improving cognitive function in Alzheimer's disease models. Hydroxytyrosol acetate has been widely used in scientific research related to Vibrio infection, arterial thrombosis, Alzheimer's disease and other related fields.

PF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC₅₀ of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain.

L-Glutamine-5-¹³C is the ¹³C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na⁺-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.

Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

Beclamide is an active molecule with anticonvulsant activity, used as an anticonvulsant drug.

Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases.

(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC₅₀=0.8 nM; β-arrestin2, EC₅₀=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.

DynaMin inhibitory peptide, myristoylated is a DynaMin inhibitor to interfere with the binding of amphiphysin with dynamin. DynaMin inhibitory peptide, myristoylated is a membrane-permeant form of the peptide that prevents endocytosis.

Glyoxal (40% w/w in water) is an α-oxoaldehyde that inhibits Aldose Reductase, Glutathione Reductase, and NADPH synthase. Glyoxal (40% w/w in water) exhibits cytotoxicity, triggers oxidative stress, induces ROS accumulation, lipid peroxidation, mitochondrial membrane potential collapse, DNA damage, apoptosis, and massive production of advanced glycation end products (AGEs). Glyoxal (40% w/w in water) depletes glutathione and activates MAPK phosphorylation. It has lower toxicity as a fixative than paraformaldehyde (PFA) and serves as a precursor for the synthesis of oxalates and dietary carcinogens. Glyoxal (40% w/w in water) is suitable for research related to calcium oxalate kidney stones, diabetes, atherosclerosis, cardiovascular diseases, retinopathy, and cataracts.

BAY-2925976 is an α2C adrenergic receptor (ARα2C) antagonist that can be used for the study of obstructive sleep apnea (OSA).

PSB-16131 is a potent inhibitor of human NTPDase2, showing non-competitive inhibition with an IC₅₀ of 539 nM. PSB-16131 can be used in the study of inflammation, neurodegenerative diseases and cancer.

Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.

Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC₅₀ of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.

SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC₅₀=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.

Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC₅₀ of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.

Amyloid-β-IN-3 (EX.113) is a selective γ-secretase inhibitor. Amyloid-β-IN-3 inhibits Aβ42 secretion in H4 cells with an EC₅₀ value of 148 nM. Amyloid-β-IN-3 regulates the γ-secretase catalytic activity to decrease Aβ42 production, thereby alleviating neurotoxicity caused by Aβ deposition. Amyloid-β-IN-3 is promising for research of Alzheimer's disease (AD).

3'-O-Methylbatatasin III shows spasmolytic activity.