Neurological Disease

CAII-IN-15 is a potent carbonic anhydrase II (CA II) inhibitor with a hCA II IC₅₀ of 10 nM. CAII-IN-15 elevates cGMP levels, releases nitric oxide, reduces oxidative stress, and exhibits neuroprotective activity in vitro. CAII-IN-15 inhibits NLRP3 inflammasome activation, reduces neuronal apoptosis. CAII-IN-15 reduces Intraocular pressure (IOP) in rabbits. CAII-IN-15 can be used for the research of glaucoma.

L-Glutamic acid (monosodium salt) (Standard) is the analytical standard of L-Glutamic acid (monosodium salt). This product is intended for research and analytical applications. L-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases.

Carbidopa (monohydrate) (Standard) is the analytical standard of Carbidopa (monohydrate). This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.

OS-3-106 is a potent, and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (K_i = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research.

YM 934 is a potassium channel opener. YM 934 inhibits neurogenic plasma leakage. YM 934 inhibits airway neurogenic inflammation.

SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect.

NLRP3-IN-38 (Compound 18) is an inhibitor for NOD-like receptor protein 3 (NLRP3), that inhibits NLRP3 inflammasome activation with an EC₅₀ of 23 nM.

Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.

Deoxysappanone B (3-Deoxysappanone B) is a homoisoflavone compound isolated from Caesalpinia sappan L (Lignum Sappan). Deoxysappanone B has anti-neuroinflammatory and neuroprotective effects and inhibits the production of neuroinflammatory mediators by blocking the IκB kinase (IKK)-NF-κB and p38/ERK MAPK pathways. Deoxysappanone B can be used in disease studies of neuritis and inflammation-related neurological damage.

5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT_2A receptor, with an EC₅₀ value of 416.9 nM and a K_i value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the 5-HT_2B receptor (EC₅₀ = 120.2 nM), D2 receptor (K_i = 1298 nM), and has no activity towards the 5-HT_2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC₅₀ = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD).

Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a potent ED₅₀ of 0.04 mmol/kg. By inhibiting Keap1-Nrf2 binding and activating the Nrf2/ARE pathway, Anticonvulsant agent 10 exerts anticonvulsant and neuroprotective effects, making it suitable for research in antiepileptic and neuroprotective studies.

Trimebutine-d₃ hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

Ectylurea, a N-acylurea, can be used in studies of tension and anxiety symptoms, has no effect on the autonomic nervous system, and has no convulsive, analgesic or antispasmodic activity in animals.

Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.

Felbinac tris (4-Biphenylacetic acid tris) is a potent analgesic agent. Felbinac tris metabolized into 4'-hydroxyfelbinac and is excreted via urine and feces. Felbinac tris has the potential for the research of post-operative pain.

STEP-IN-1 (Compound 14b) is a potent and selective STEP inhibitor with an IC₅₀ of 5.27 μM. STEP-IN-1 has a neuroprotective effect, which can protect nerve cells from glutamate-induced toxicity, reduce cellular ROS accumulation, and inhibit apoptosis. STEP-IN-1 can be used in the study of neurodegenerative diseases.

mcK6A1 is an inhibitor for the aggregation of amyloid-β (Aβ), that selectively binds to the 16KLVFFA21 segment of Aβ42, forms an extended β-folded structure, and inhibits the formation of Aβ42 oligomers. mcK6A1 can be used in research of Alzheimer's disease and other amyloid-related diseases.

threo-Anethole glycol (Compound 12) is an aromatic diol compound found in Foeniculi Fructus. threo-Anethole glycol has potential antioxidant activity and can be used for the researches of inflammation, cardiovascular and neurological disease.

5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC₅₀s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.

Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC₅₀ value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.