Neuronal Signaling

Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.

Tolterodine tartrate (Detrol LA) is a muscarinic receptor antagonist which is used for the treatment of urinary incontinence.

Varenicline is a nicotinic receptor partial agonist.

GW791343 HCl acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.

Tau protein (592-597), human TFA is a peptide fragment of human Tau protein. The dysfunction of Tau protein is involved in neurodegeneration and dementia.

Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.

CGP7930 (3-(3',5'-Di-tert-butyl-4'-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons.

Acetly-β Amyloid (15-20), Amide is a peptides fragment. Acetly-β Amyloid (15-20), Amide inhibits the β-sheet formation and stabilizes structure of Aβ (1-40) peptide. Acetly-β Amyloid (15-20), Amide can be used in study Alzheimer's disease.

α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.

Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.

COG 133 TFA is a fragment of Apolipoprotein E (APOE) peptide. COG 133 TFA competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 TFA is also a nAChR antagonist with an IC50 of 445 nM.

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

β-Amyloid (35-42) is a peptide consisting of amino acid of 35 to 42 of beta amyloid protein.

β-Amyloid peptide(16-20) is a amino acid sequences (KLVFF) of Amyloid-β (Abeta). β-Amyloid peptide(16-20) is an effective inhibitor of Abeta fibril formation, with RG-/-GR-NH2 residues added at N- and C-terminal ends to aid solubility).

Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction.

DQP-1105 is a negative allosteric modulator of the GluN2C/D NMDA receptor inhibiting receptor function more potently when glutamate is present .

Cgs 20625 is a benzodiazepine receptor agonist.

Ro 19-4603 is a benzodiazepine receptor inverse agonist.

DNQX Disodium is a water-soluble form of selective non-NMDA receptor antagonist DNQX.

Distigmine Bromide, also known as Ubretid and BC-51, is an acetylcholinesterase inhibitor used for the treatment of underactive neurogenic bladder and myasthenia gravis.

SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.

Gabazine free base is a specific GABA receptor antagonist. Does not affect GABA-transaminase or glutamate-decarboxylase activitites.

Tracazolate is a pyrazolopyridine anxiolytic known to interact with gamma-aminobutyric acid (GABA)(A) receptors, adenosine receptors, and phosphodiesterases.

GABAA Modulator I is novel modulator of the GABAA receptor complex, and in particular for combating anxiety and related diseases.

rac-BHFF is a selective GABAB receptor agonist.

NSC 102533 is a potent antagonist of the purinergic P2X7 receptor, a ligand-gated ion channel involved in inflammation and immune regulation. It effectively inhibits ATP-induced dye uptake in HEK293 cells expressing human P2X7 receptors with an IC₅₀ of 22.4 nM. NSC 102533 also suppresses ATP-induced IL-1β secretion in human THP-1 monocytes and primary mouse peritoneal macrophages, with IC₅₀ values of 9.8 nM and 11.2 nM, respectively, demonstrating strong anti-inflammatory activity.

In addition to its immunomodulatory effects, NSC 102533 exhibits antivenom potential by inhibiting Bothrops atrox venom proteolysis in a concentration-dependent manner. In in vivo studies, intradermal administration of NSC 102533 (3 mg/kg) significantly reduces skin hemorrhage induced by B. atrox and B. jararaca venom and attenuates carrageenan-induced paw edema in mice at doses between 0.01 and 1 mg/kg. These properties highlight NSC 102533 as a valuable pharmacological tool for studying P2X7 receptor–mediated inflammatory responses and venom-induced pathology.

Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM.

GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.

Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.

BNC210 (H-Ile-Trp-OH; IW-2143) is a α7 nAChR negative allosteric modulator. BNC210 has potent activity in animal models of anxiety and depression.

Pamicogrel (KBT3022) is a cyclooxygenase (COX) inhibitor.

C004019 is a small-molecule PROTAC designed to target tau, functioning as a tau scavenger. This compound effectively recruits tau and E3 ligase, promoting the ubiquitination and proteasome-dependent degradation of tau proteins. C004019 has demonstrated the potential to enhance synaptic and cognitive functions in models of Alzheimer's disease, making it a valuable tool for research into Alzheimer's and tau protein-related pathologies.

RSS0680 is a small noncoding RNA (sRNA) that targets the ribosome binding site (RBS) of mRNA, functioning as a PROTAC to facilitate the degradation of various protein kinases. By competitively binding to the RBS through its conserved anti-Shine-Dalgarno sequence, RSS0680 inhibits the translation initiation of target genes. Key biological activities include the degradation of kinases such as AAK1, CDK1, and MAPK6, making it a valuable tool for investigating diseases associated with dysregulated kinase activity. Additionally, RSS0680 plays a role in bacterial oxidative stress defense and can enhance resistance to heat shock and oxidative damage by modulating metabolic pathways.

OSMI-1 is a potent cell-permeable inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 2.7 μM. This compound effectively decreases protein O-linked N-acetylglucosamine (O-GlcNAcylation) levels in various mammalian cell lines while maintaining the integrity of cell surface N- and O-linked glycans. OSMI-1 serves as a valuable tool for studying the regulatory roles of O-GlcNAcylation in cellular processes and diseases.

Scyllo-Inositol is an aggregation inhibitor that targets misfolded proteins, specifically α-synuclein and Amyloid-β. It effectively stabilizes non-toxic oligomers, preventing their conversion into toxic fibrils, thus supporting protein homeostasis and providing neuroprotective effects. By binding to the hydrophobic regions of pathogenic proteins, Scyllo-Inositol inhibits protein aggregation and enhances lysosome- and proteasome-mediated degradation pathways, ultimately reducing neurotoxicity. This compound is valuable for researching neurodegenerative diseases, including Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease.

Hoechst 34580 tetrahydrochloride is a nuclear marker dye that selectively targets A/T-rich double-stranded DNA. This compound exhibits enhanced fluorescence intensity when bound to nucleic acids, making it valuable for live cell labeling applications. As the pH of the solution increases, the fluorescence intensity of Hoechst 34580 also increases, providing a reliable tool for studying cellular dynamics, DNA distribution, and nuclear morphology in real-time. This reagent is particularly useful in research focused on amyloid-β and related neurodegenerative processes.

Pilocarpine Hydrochloride is a selective agonist for the M3 muscarinic acetylcholine receptor (mAChR). It plays a significant role in stimulating glandular secretion, particularly in the treatment of dry mouth and glaucoma. This compound is valuable in research focused on neuropharmacology, as well as studies investigating cholinergic signaling and its implications in various physiological processes.

RGH-857 acts as a selective and potent positive allosteric modulator of nicotinic α7 receptors. It demonstrates effectiveness in ameliorating amnesia and is valuable in studies related to Alzheimer's disease. This compound can facilitate research into cognitive impairment and potential therapeutic interventions in neurodegenerative disorders.

X-34 is a lipophilic fluorescent derivative of Congo red, characterized by its bright yellow-green fluorescence. It selectively stains neuritic and diffuse plaques, neurofibrillary tangles, neuropil threads, and cerebrovascular amyloid in brain tissue. This reagent is widely utilized in research focused on Alzheimer's disease to facilitate the study of these key pathological features.

Iminostilbene is a well-characterized inhibitor of COX2 (Cyclooxygenase-2) with additional activity against PKM2 (Pyruvate Kinase M2). This compound effectively reduces the expression of COX2 and iNOS, as well as the release of pro-inflammatory cytokines such as IL-1β, IL-6, TNF-α, and MCP-1 in macrophages. Its ability to mitigate macrophage-mediated inflammatory responses makes iminostilbene a valuable reagent for investigating mechanisms of inflammation regulation, cardiovascular disease, including myocardial ischemia/reperfusion injury, and immune-related disorders.

Primidone-d5 is a deuterium-labeled analog of Primidone, primarily known for its inhibitory action on the transient receptor potential melastatin 3 (TRPM3) channel, with an IC50 value of 0.6 μM. This reagent also inhibits receptor-interacting protein (RIP) kinase and voltage-gated sodium channels, while acting as an antagonist at the GABA receptor. Primidone-d5 is valuable for research in pain management and seizure disorders, enabling studies focused on its analgesic and anticonvulsant properties.

CS640 is a selective inhibitor of calmodulin-dependent kinase 1D (CaMK1D) with additional activity against several other kinases, including CaMK1B, CaMK1A, and MEK5, demonstrating IC50 values of 8 nM, 3 nM, 1 nM, and 25 nM, respectively. This compound effectively inhibits Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, making it valuable for studies on tau pathology. While CS640 does not provide protective effects against Aβ-induced neurotoxicity in primary mouse cortical neurons, it is useful for research focusing on the mechanisms of Alzheimer's disease.

(Rac)-PEAQX is an NMDA receptor antagonist that effectively modulates synaptic transmission by inhibiting NMDA receptor activity. It has demonstrated the ability to activate caspase-3, inducing apoptotic pathways in cortical striatal slice cultures. This compound is valuable for research applications focusing on neurodegenerative diseases, synaptic plasticity, and mechanisms of neuronal apoptosis.

Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis.

Neuroprotective Agent 15 is a selective butyrylcholinesterase (BChE) inhibitor with IC50 values of 2.6 μM for BChE and 114.3 μM for acetylcholinesterase (AChE). This compound exhibits cannabinoid CB2 receptor agonistic activity, contributing to its neuroprotective properties. Neuroprotective Agent 15 has been shown to reduce cell death, alleviate LDH release, and inhibit Caspase-3/7 activity, thereby diminishing apoptosis. Additionally, it mitigates the formation of superoxide free radicals, preserves cell morphology, and lowers oxidative stress levels, making it a valuable tool for research into neurodegenerative diseases such as Alzheimer's and Parkinson's disease.

NDs-IN-1 is a non-covalent multi-target inhibitor designed to inhibit the activities of key enzymes including human beta-secretase 1 (hBACE-1), human acetylcholinesterase (hAChE), and human monoamine oxidase B (hMAO-B). This compound is primarily utilized in research focused on neurodegenerative diseases, offering potential avenues for understanding disease mechanisms and developing therapeutic strategies.

δ-Secretase inhibitor 11 is a potent and selective inhibitor targeting δ-secretase, displaying an IC50 of 0.7 μM. This compound effectively interacts with both the active and allosteric sites of δ-secretase, resulting in the attenuation of tau and amyloid precursor protein cleavage. Its oral bioavailability and blood-brain barrier penetration make it suitable for in vivo studies, particularly in transgenic mouse models. δ-Secretase inhibitor 11 is a valuable tool for Alzheimer's disease research, facilitating investigations into the mechanisms underlying synaptic dysfunction and cognitive impairments.

AChE-IN-105 is a potent mixed inhibitor of acetylcholinesterase (AChE) with an IC50 value of 5.02 μM. It exhibits significant antioxidant properties by scavenging reactive oxygen species (ROS) and mitigating hydrogen peroxide-induced activation of Caspase-3, while also downregulating the Nrf2-ARE pathway. In preclinical studies, AChE-IN-105 demonstrated the ability to prevent memory deficits in a zebrafish model of scopolamine-induced cognitive dysfunction. This compound is valuable for research focused on Alzheimer's disease and cognitive impairment mechanisms.

(E)-Ethyl p-methoxycinnamate is a COX inhibitor that exhibits significant anti-inflammatory properties. Isolated from Kaempferia galangal, this compound demonstrates both anti-neoplastic and anti-microbial activities. In vitro studies reveal that (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 with IC50 values of 1.12 μM and 0.83 μM, respectively, making it a valuable reagent for research in inflammatory and cancer-related studies.