Neurological Disease

AChE/BChE-IN-34 is an acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor with IC₅₀s of 5.97 μM and 4.57 μM, respectively. AChE/BChE-IN-34 functions as an antioxidant, oxidative stress inhibitor, reduces MDA levels, and elevates SOD and catalase in hippocampal tissue. AChE/BChE-IN-34 acts as a cognitive function enhancer, improves learning and memory in a Scopolamine (HY-N0296)-induced animal model. AChE/BChE-IN-34 is non-toxic in neuroblastoma cells across a specified concentration range. AChE/BChE-IN-34 can be used for the research of Alzheimer's disease.

S-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) is a blood-brain barrier (BBB) penetrant NOS inhibitor with IC₅₀ values of 0.66, 0.75 and 0.29 μM against mouse spinal cord, cerebellar, bovine aortic and porcine endothelial cell NOS. S-Isopropylisothiourea exhibits a significant blood pressure-raising effect without damaging the perfusion of vital organs and can also inhibit the late-phase pain response induced by formalin. S-Isopropylisothiourea hydrobromide is used in the researchs for hemorrhagic shock and pain response based on NOS.

VIP Guinea pig TFA (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guinea pig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function.

YMRF-NH2 is a neuropeptide. YMRF-NH2 binds to FMRFa-R with an EC₅₀ value of 31 nM.

PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin (mHTT) PROTAC degrader. PROTAC mHTT Degrader-1 specifically recognizes pathogenic mHTT aggregates and recruits Cereblon (CRBN), thereby inducing ubiquitination and proteasomal degradation of mHTT. PROTAC mHTT Degrader-1 alleviates mHTT-induced cytotoxicity and neuroinflammation. In the R6/2 Huntington's disease mouse model, PROTAC mHTT Degrader-1 reduces cerebral protein aggregation levels and improves body weight, motor coordination and survival rate of animals. PROTAC mHTT Degrader-1 can be used for research on PROTAC therapies for Huntington's disease and other neurodegenerative diseases.

Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC (Salmiac, meets analytical specification of Ph. Eur. BP USP FCC) is an inhibitor of Slc26a4 and SMAD2. Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC reduces the protein expression level of Slc26a4 in lung tissue, and attenuates ozone-induced increases in proinflammatory cytokines, inflammatory cells, pulmonary resistance, goblet cell hyperplasia, peribronchial inflammation and thiocyanate levels in mouse tissues and bronchoalveolar lavage fluid. Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC decreases the level of phosphorylated SMAD2, inhibits autophagy by reducing autophagy-related proteins, and enhances Cisplatin (HY-17394)-induced cancer cell apoptosis and DNA double-strand breaks. Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC also inhibits the TCA cycle, reduces ATP production, increases glucose utilization, regulates the levels of lactic acid, glutamic acid and ATP, and induces morphological degeneration of neuroblastoma cells. Ammonium chloride, meets analytical specification of Ph. Eur. BP USP FCC can be used in studies related to ozone-induced airway injury, hepatocellular carcinoma, human cervical cancer, hepatic encephalopathy, Reye syndrome, epilepsy and neurodegenerative diseases.

α-Synuclein-IN-18 (Compound Mol D) is an inhibitor of the autocatalytic proliferation of α-Synuclein aggregate. α-Synuclein-IN-18 can specifically bind to the conserved binding pocket on the surface of α-synuclein fibrils. α-Synuclein-IN-18 can delay the aggregation process of α-synuclein, extend the aggregation T_1/2 by three times. α-Synuclein-IN-18 can reduce the generation flux of α-synuclein toxic oligomers, thereby alleviating the neurotoxicity. α-Synuclein-IN-18 can be used for research of Parkinson’sdisease.

Bacopaside N2 is a diglycosidic saponin.

Trichosanthis fructus extract is an extract of Trichosanthis fructus that can be used in research on angina pectoris, heart failure, myocardial infarction, pulmonary heart disease, and cerebral ischemia.

PDE5/CA-IN-1 is a dual PDE5 and carbonic anhydrase (CA) inhibitor, with IC₅₀ values of 0.41, 38.4, and 9.1 nM against PDE5, hCA II, and hCA VA, respectively. PDE5/CA-IN-1 inhibits multiple hCA subtypes associated with Alzheimer's disease. As a cytoprotective agent and oxidative stress alleviator, PDE5/CA-IN-1 reduces oxidative stress, and prevents recognition memory and working memory impairments. PDE5/CA-IN-1 is available for the research of Alzheimer's disease.

Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC₅₀s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.

GSK-3β inhibitor 18 (compound 2) is a potent inhibitor of GSK-3β, with the IC₅₀ of 0.0021 μM.

H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC₅₀ = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC₅₀ = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED₅₀ = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy.

NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC₅₀ value of 32 nM, similar to NT160 (HY-149285) (IC₅₀= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases.

5-TAMRA-Amyloid β-Protein (1-40) is a fluorescent (TAMRA)-labeled Amyloid β-Protein (1-40), Abs/Em=544/572 nm.

CP 93129 is a potent and selective 5-HT_1B agonist. CP 93129 has the potential for the research of Parkinson's disease.

NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.

Qingyangshengenin A, a C-21 steroidal glycoside isolated from the roots of Cynanchum otophyllum Schneid, has antiepileptic activity.

Prolactin-Releasing Peptide (12-31), bovine is a peptide fragment of prolactin-releasing peptide (PrRP). PrRP is RF-amide peptides expressed in brain areas involved in pain modulation. Prolactin-Releasing Peptide (12-31), bovine can be used for the research of nervous system disease.

Trebenzomine (CI-686 free base) is a centrally acting psychotropic compound. Trebenzomine has both neuroleptic and stimulant activity. Trebenzomine potentiates Methamphetamine-induced self-stimulation. Trebenzomine reduces septal hyperirritability, suppression of conditioned avoidance behavior, blocks Apomorphine (HY-12723)-induced emesis in dogs.