Catalog No.
Product Name
Application
Product Information
Citations
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PN-1 Agonist
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1), promoting its expression through the cAMP-PKA-Sp1 signaling pathway, which enhances granule biogenesis in endocrine cells. This compound is instrumental in studying the regulation of secretory functions and demonstrates selectivity for β-adrenergic receptors. By interacting with β1-adrenergic receptors, Serpinin activates the AC-cAMP-PKA pathway, crucial for regulating myocardial systolic and diastolic function. Additionally, pGlu-serpinin has been shown to upregulate Bcl2 mRNA transcription, contributing to its neuroprotective effects. -
Anti-platelet Aggregation Agent
Antiplatelet agent 3 is a potent anti-platelet aggregation agent that inhibits platelet aggregation induced by ADP, AA, and COL, with IC50 values of 2.55, 3.22, and 2.09 mg/mL, respectively. This compound demonstrates significant biological activity advantageous for elucidating mechanisms involved in thrombosis and other cardiovascular conditions. Antiplatelet agent 3 is suitable for use in cardiovascular disease research, providing insights into therapeutic strategies for managing platelet-related disorders. -
β-Glucuronidase Inhibitor
β-Glucuronidase-IN-5 is a selective inhibitor of β-glucuronidase with an IC50 value of 39.8 μM. This compound demonstrates low cytotoxicity in PC-3 cells, with an IC50 greater than 30 μM, and shows no affinity for adenosine receptors A₁ and A₂A. β-Glucuronidase-IN-5 is useful for investigating diseases associated with overexpression of β-glucuronidase, including colon cancer, arthritis, and complications related to AIDS. -
PAF C-16 Precursor/Metabolite
Lyso-PAF C-16 is a key precursor and metabolite of 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine (PAF C-16). It serves as a substrate in the remodeling pathway for the formation of PAF C-16 and is also involved in the selective acylation with arachidonic acid through a CoA-independent transacylase. This compound is beneficial for research into lipid metabolism and the roles of bioactive lipids in various biological processes. -
PAFAH1b2/1b3 Inhibitor
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3, demonstrating significant impairment of cancer cell survival. With IC50 values of approximately 40 nM for PAFAH1b2 and 900 nM for PAFAH1b3, P11 is a valuable tool for investigating the role of these enzymes in cancer biology and related research applications, including studies focused on cell proliferation and apoptosis. -
Sigma Receptor Ligand
Caprospinol is a potent σ-1 receptor ligand that exhibits neuroprotective properties through multiple mechanisms. It effectively binds to β-amyloid protein (Aβ(42)), interacts with the mitochondrial respiratory chain, and facilitates the clearance of Aβ(42) monomers. Caprospinol is capable of crossing the blood-brain barrier, thereby showing promise in restoring cognitive function and inhibiting the progression of Alzheimer's disease. Its diverse biological activities make it a valuable tool for research in neurodegenerative disorders. -
Anticholinergic
Piperilate is an anticholinergic agent that functions primarily as a PAF antagonist through its hetrazepine derivatives. This compound exhibits significant biological activity in the treatment of bronchial asthma and demonstrates hypotensive effects. Additionally, Piperilate has been shown to effectively rescue mice from organophosphate poisoning, making it a valuable reagent for research into respiratory conditions and toxicology. -
DA/NE/5-HT Inhibitor
Tesofensine is a triple monoamine reuptake inhibitor targeting dopamine (DA), norepinephrine (NE), and serotonin (5-HT). It effectively inhibits the reuptake of these neurotransmitters in the synaptic cleft, exhibiting IC50 values of 6.5 nM for DA, 1.7 nM for NE, and 11 nM for 5-HT. Tesofensine is primarily studied for its potential as an anti-obesity agent and may be useful in related central nervous system research applications. -
MAO-A And 5-HT-uptake Inhibitor
Sercloremine hydrochloride is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) and serotonin (5-HT) uptake. This compound is primarily utilized in research related to depression, offering insights into the modulation of serotonin levels and its effects on mood regulation. Its dual mechanism of action makes it valuable for exploring therapeutic approaches in depressive disorders. -
5-HT Reuptake Inhibitor
Clomipramine is a potent 5-HT reuptake inhibitor with an IC50 value of 1.5 nM. As a tricyclic antidepressant, it is primarily utilized in research investigating the mechanisms of depression and obsessive-compulsive disorder (OCD). Its ability to influence serotonin levels makes it a valuable tool for studying various neuropsychiatric conditions. -
5-HT2A Antagonist
Glemanserin is a potent and selective antagonist for the serotonin receptor 5-HT2A, exhibiting nanomolar affinity in various species (Ki values of 2.89, 0.54, and 2.5 nM for rat, rabbit, and human 5-HT2A, respectively). This compound is primarily utilized in neuropharmacological research to study the role of 5-HT2A receptors in various physiological and pathological conditions. Its antagonistic activity contributes to investigations into mood disorders, anxiety, and other CNS-related ailments. -
5-HT/NE Reuptake Inhibitor
Dextromilnacipran is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor, derived from the enantiomeric form of milnacipran. This compound also functions as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 value of 3.4 μM. Dextromilnacipran is primarily utilized in research applications targeting mood disorders and neuropharmacology, facilitating investigations into its psychiatric and physiological effects. -
5-HT Uptake Blocker
Indalpine, a selective 5-HT uptake blocker, demonstrates significant potency in inhibiting serotonin transport. With an IC50 value of 36 μM, it effectively displaces ^3H-5-HT bound to brain membranes. This compound may have applications in the study of antidepressant mechanisms and is valuable for research in neuropharmacology. -
Stable Isotope
Dextromilnacipran-d6 is a deuterium-labeled analog of Dextromilnacipran, a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. This compound also acts as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 of 3.4 μM. Dextromilnacipran-d6 is a valuable tool for metabolic and pharmacokinetic studies, providing insights into the behavior and efficacy of 5-HT/NE reuptake inhibitors in various research contexts. -
Noradrenaline And 5-HT Uptake Blocker
Clemeprol is an orally active noradrenaline and 5-HT uptake blocker. It effectively inhibits the depletion of brain noradrenaline induced by 6-Hydroxydopamine and demonstrates a dose-dependent inhibition of reserpine-induced hypothermia. Clemeprol is applicable in the investigation of depression and related neurochemical pathways. -
5-HT1 Agonist
2-Aminotetralin is a selective agonist of the serotonin 5-HT1 receptor subtypes, including 5-HT1A, 5-HT1B, and 5-HT1D. This compound demonstrates high affinity, with a Ki value of 25 nM or lower, and exhibits significant stereoselectivity, showing over a 50-fold preference for specific receptor configurations. 2-Aminotetralin is utilized in research exploring serotonin signaling pathways and their implications in neuropharmacology and mood disorders. -
5-HT Transporter Inhibitor
6-Nitroquipazine is a highly potent and selective inhibitor of the serotonin transporter (5-HT transporter), exhibiting a Ki value of 0.17 nM. This compound significantly impacts serotonin reuptake, making it a valuable tool for investigating the pathophysiology and treatment of psychiatric disorders, including depression. Its ability to modulate serotonin levels can be instrumental in research aimed at understanding mood regulation and therapeutic interventions in related conditions. -
S1R Agonist
S1R Agonist 3 is a highly selective sigma-1 receptor (S1R) agonist with a binding affinity (Ki) of 1.5 nM. It demonstrates the capability to reduce hyperlocomotion in wfs1abKO zebrafish larvae while leaving locomotion unaltered in wildtype wfs1abWT zebrafish. Additionally, S1R Agonist 3 effectively reverses learning and memory deficits induced by the Aβ25-35 peptide, highlighting its potential utility in Alzheimer’s disease research. -
Vesicular Acetylcholine Transport Inhibitor
(±)-Vesamicol hydrochloride is a potent inhibitor of vesicular acetylcholine transport, exhibiting a Ki value of 2 nM. Additionally, it demonstrates a high affinity for σ1 and σ2 receptors, with Ki values of 26 nM and 34 nM, respectively. This compound is valuable for research into cholinergic signaling and receptor interactions, facilitating studies on neurological disorders and synaptic transmission mechanisms. -
Sigma 1 Receptor Antagonist
BD1063 dihydrochloride is a potent and selective antagonist of the sigma 1 receptor. This compound plays a significant role in modulating various neurological processes and exhibits potential neuroprotective effects. BD1063 is valuable in studies investigating neurodegenerative diseases, pain management, and the modulation of mood disorders. -
Sigma-2 Receptor Ligand
CM398 is a selective sigma-2 receptor ligand that demonstrates a high binding affinity (Ki = 0.43 nM) while maintaining a 1000-fold selectivity over the sigma-1 receptor. In addition to its primary target, CM398 exhibits appreciable affinity for dopamine (Ki = 32.90 nM) and serotonin (Ki = 244.2 nM) transporters. This compound has shown promising anti-inflammatory and analgesic properties in preclinical studies, specifically within the formalin model of inflammatory pain in mice, making it a valuable tool for research in pain management and neuropharmacology. -
σ1 Receptor Ligand
PD 144418 is a potent and selective sigma 1 (σ1) receptor ligand, exhibiting a high affinity with a Ki value of 0.08 nM for σ1 and significantly lower affinity of 1377 nM for σ2 receptors. This compound demonstrates minimal interaction with other receptors, ion channels, and enzymes, ensuring specificity in its action. PD 144418 has shown potential antipsychotic properties, making it a valuable tool for research into psychiatric disorders and sigma receptor biology. -
σ2 Receptor Ligand
WLB-89462 is a selective σ2 receptor ligand, exhibiting an affinity (Ki) of 13 nM. This compound demonstrates neuroprotective activity, effectively improving short-term memory impairment caused by Aβ peptide in rodent models. Additionally, WLB-89462 possesses a favorable ADMET profile, characterized by good solubility, lack of CYP inhibition, metabolic stability, high permeability, and significant brain penetration, making it a valuable tool for research in neurodegenerative diseases. -
Sigma (σ) Receptor Agonist
Opipramol is a sigma (σ) receptor agonist that exhibits potent interaction with sigma recognition sites, demonstrating a Ki value of 50 nM. This atypical tricyclic antidepressant (TCA) is primarily utilized in research focused on generalized anxiety disorder (GAD). Its mechanism of action may contribute to modulating anxiety-related behaviors, making it a valuable compound for studies investigating novel therapeutic approaches in anxiety disorders. -
Sigma-1 Receptor Antagonist
IPAG is a potent antagonist of the sigma-1 receptor, exhibiting a pKi of 4.3. It has been shown to induce apoptosis in various cell types, making it a valuable tool for research in cancer biology and neuroprotection. Applications include the study of sigma-1 receptor signaling pathways and potential therapeutic strategies targeting these mechanisms. -
Sigma Ligand
Panamesine is a selective sigma receptor ligand with a high affinity of IC50 6 nM for sigma binding sites. This compound exhibits potential as an atypical neuroleptic agent, making it of interest in neuropharmacological research. Its unique binding properties may provide insights into the therapeutic mechanisms of sigma receptor modulation in various neurological disorders. -
Sigma Receptor Antagonist
DuP 734 is a selective sigma receptor antagonist that also targets the 5-HT2 receptor with high potency. It exhibits weak affinity for D2 receptors, suggesting a profile that may offer antipsychotic effects while minimizing motor side effects commonly associated with traditional neuroleptics. This compound is valuable for research in neuropharmacology and may aid in the exploration of novel treatments for psychiatric disorders. -
Sigma-1 Receptor Antagonist
EST64454 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting a Ki value of 22 nM. This compound shows promise in the investigation of pain mechanisms and may facilitate new research into pain management therapies. Its oral bioavailability allows for convenient applications in preclinical studies. -
Sigma Receptor Antagonist
Trifluperidol hydrochloride is a potent Sigma-1 receptor antagonist, exhibiting a Ki value of 3.3 nM. This compound is primarily utilized in research focused on psychotic disorders, facilitating investigations into neuropharmacological mechanisms and potential therapeutic strategies. Its inhibitory action on the Sigma-1 receptor supports studies related to mood and psychotic disorders. -
Sigma Receptor Inhibitor
KB-5492 free base is a selective inhibitor of sigma receptors, demonstrating potent activity by inhibiting specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound exhibits anti-ulcer properties, making it valuable for research in gastrointestinal disorders and related therapeutic applications. Its mechanism of action also suggests potential implications in neuropharmacology and pain management studies. -
σ1 R Antagonist
Sigma-1 Receptor Antagonist 1 (compound 137) is a selective antagonist of the sigma-1 receptor (σ1R), demonstrating a high binding affinity with a Ki value of 1.06 nM. This compound exhibits notable antineuropathic pain activity, making it a promising candidate for research into therapeutic interventions for neuropathic pain. Its specificity for σ1R positions it as a valuable tool in understanding the biological functions and potential clinical applications of sigma-1 receptor modulation. -
Sigma Receptor
PD 144418 oxalate is a selective and potent ligand for the sigma 1 (σ1) receptor, demonstrating a high binding affinity with a Ki value of 0.08 nM. Its selectivity is underscored by minimal affinity for sigma 2 (σ2) and other biological targets, including receptors, ion channels, and enzymes. This compound has potential applications in studying antipsychotic mechanisms and could serve as a valuable tool in neuropharmacological research. -
σ Receptor Antagonist
BD-1008 is a potent nonselective σ receptor antagonist, exhibiting Ki values of 2 nM and 8 nM for σ1 and σ2 receptors, respectively. With minimal affinity for the D2 receptor (Ki = 1112 nM) and negligible binding to the dopamine transporter (Ki > 10,000 nM), BD-1008 effectively antagonizes dopamine release in the nucleus accumbens shell region through σ₂ receptor blockade. This compound serves as a valuable tool for investigating addiction therapies targeting σ receptors. -
S1R Antagonist
AB21 hydrochloride is a potent and selective antagonist of the sigma-1 receptor (S1R), exhibiting a Ki of 13 nM for S1R and 102 nM for S2R. This compound effectively reduces mechanical hypersensitivity, making it a valuable tool for research in pain mechanisms and neuropharmacology. Its application in studying the sigma receptor's role in various biological processes highlights its significance in addressing pain-related conditions and therapeutic interventions. -
S1R Agonist
S1R Agonist 1 is a selective sigma-1 receptor (S1R) agonist, demonstrating a binding affinity (Ki) of 0.93 nM for S1R and 72 nM for S2R. This compound exhibits neuroprotective effects against reactive oxygen species (ROS) and N-methyl-D-aspartate (NMDA)-induced neurotoxicity. It is useful in research applications aimed at understanding neurodegenerative diseases and neuroprotection mechanisms. -
S1R Agonist
S1R agonist 1 hydrochloride is a selective agonist of the sigma-1 receptor (S1R), demonstrating a binding affinity with a Ki of 0.93 nM for S1R and 72 nM for the sigma-2 receptor (S2R). This compound displays neuroprotective properties against reactive oxygen species (ROS) and NMDA-induced neurotoxicity. S1R agonist 1 hydrochloride is applicable in research focused on neurodegenerative conditions and the modulation of cellular stress responses. -
Sigma Receptor Inhibitor
KB-5492 anhydrous is a selective inhibitor of the sigma receptor, demonstrating inhibition of specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding with an IC50 of 3.15 μM. This compound has been identified for its potential application as an anti-ulcer agent, making it relevant for research in gastrointestinal disorders and sigma receptor pharmacology. Its activity underscores the significance of sigma receptors in various biological processes, providing valuable insights for therapeutic exploration. -
σ-Receptor Ligand
Igmesine hydrochloride is a potent σ-receptor ligand that exhibits the ability to inhibit colonic electromechanical activity stimulated by emotional stress. This compound effectively counteracts the enhancement of colonic motility induced by dopamine and centrally injected D1 or D2 receptor agonists. Additionally, Igmesine hydrochloride disrupts the colonic motility responses prompted by corticotropin-releasing factor (CRF), likely through mechanisms involving central cholecystokinin (CCK) release or activation of supraspinal CCK pathways, making it a valuable tool for studying gastrointestinal responses to stress and neurotransmitter signaling. -
σ2 Receptor/Tmem97 Agonist
UKH-1114 is a selective agonist for the sigma-2 receptor, specifically targeting TMEM97, with affinities of 1279 nM and 46 nM for σ1R and σ2R/TMEM97, respectively. This compound demonstrates remarkable selectivity, displaying minimal affinity for over 50 other receptors and ion channels. UKH-1114 has been shown to effectively alleviate mechanical hypersensitivity induced by spared nerve injury (SNI) while minimizing the risk of motor impairment. It serves as a valuable tool for investigating mechanisms of neuropathic pain. -
S1R Agonist
S1R Agonist 2 is a selective sigma-1 receptor (S1R) agonist, demonstrating a binding affinity of 1.1 nM for S1R and 88 nM for sigma-2 receptor (S2R). This compound exhibits significant neuroprotective effects against reactive oxygen species (ROS) and N-methyl-D-aspartate (NMDA)-induced neurotoxicity. Due to its targeted action on the S1R, S1R Agonist 2 is valuable for research focusing on neurodegenerative diseases and neuronal protection mechanisms. -
Sigma-1 Receptor Modulator
Convolamine is a sigma-1 receptor modulator derived from Convolvulus pluricaulis. It demonstrates positive modulation of the sigma-1 receptor with an IC50 of 289 nM. This compound exhibits notable cognitive-enhancing and neuroprotective activities, making it a valuable tool for research into neurological disorders and cognitive function enhancement. -
σ Receptor Antagonist
BD-1008 dihydrobromide is a nonselective σ receptor antagonist, exhibiting Ki values of 2 nM for the σ1 receptor and 8 nM for the σ2 receptor. It demonstrates minimal affinity for the D2 receptor (Ki = 1112 nM) and very low affinity for the dopamine transporter (DAT) (Ki > 10,000 nM). BD-1008 dihydrobromide effectively antagonizes dopamine release in the shell region of the nucleus accumbens via σ₂ receptor inhibition and interferes with the self-administration of σ agonists. This compound is valuable for research in addiction therapy targeting σ receptors. -
Antipsychotic/Antianxiety Agent
Umespirone is an investigational compound that functions primarily as an antipsychotic and antianxiety agent. It selectively targets serotonin receptors, contributing to its anxiolytic and neuroleptic effects. Umespirone is being explored for its potential to alleviate symptoms associated with anxiety disorders and schizophrenia, providing insights into neuropharmacological mechanisms. Its unique profile supports research in the development of new therapeutic strategies for mental health conditions. -
Sigma-2 Receptor Agonist
Siramesine fumarate is a potent sigma-2 receptor agonist with a subnanomolar affinity for sigma-2 receptors (IC50 = 0.12 nM) and a 140-fold selectivity over sigma-1 receptors (IC50 = 17 nM). This compound induces cell death through the destabilization of mitochondria without affecting lysosomes. Siramesine fumarate has demonstrated significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and the study of sigma receptor biology. -
PET Tracer
SYB4 is a positron emission tomography (PET) tracer that selectively targets the Sigma-2 receptor. Its primary application lies in neuroimaging, allowing for the visualization of Sigma-2 receptor distribution in the brains of nonhuman primates. This compound is valuable for studying neurobiological processes and may assist in understanding various neurological disorders. -
S1R Inhibitor
CM304 is a potent sigma-1 receptor (S1R) inhibitor. It demonstrates significant neuroprotective effects by mitigating drug-induced convulsions in rat models. This compound is valuable for research focused on neurological disorders and the modulation of synaptic functions associated with S1R activity. -
Sigma-1 Receptor Antagonist
EST64454 is a selective sigma-1 receptor antagonist with a Ki value of 22 nM, demonstrating oral bioactivity. This compound is useful for investigating pain mechanisms and signaling pathways associated with sigma-1 receptor activity. Its application in research can provide insights into pain modulation and potential therapeutic interventions. -
Ligand
KSCM-11 is a selective ligand for the sigma receptor, functioning as a modulator of sigma receptor activity. This compound exhibits significant potential in neuroscience research, contributing to studies on neuroprotection, pain management, and the modulation of psychotropic effects. Its targeted action on sigma receptors makes it a valuable tool for exploring therapeutic avenues in neurological disorders. -
σ ligand
L-693403 maleate is a highly selective sigma receptor ligand with strong binding affinity. This compound serves as an important tool for investigating sigma receptor-mediated pathways and their potential implications in various physiological diseases. It is suitable for research applications focused on understanding the role of sigma receptors in neurobiology and pharmacology.
