Catalog No.
Product Name
Application
Product Information
Citations
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Sigma-2 receptor agonist
Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. -
sigma-1 receptor antagonist
S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ?? 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. -
sigma 1 receptor(σ1R) agonist
SA4503 is a selective sigma 1 receptor(ς1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor. -
Sigma-2 receptor agonist
Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. -
Sigma-1 antagonist
BD-1047 2HBr is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. -
sigma1 receptor agonist
Anavex2-73 is a muscarinic/moderate sigma1 receptor agonist that alleviated the scopolamine- and dizocilpine-induced learning impairments. CAS: 195615-83-9 (Free base) 195615-84-0 (HCl) -
sigma-2 (σ2) receptor ligand
Glycerol phenylbutyrate is a sigma-2 (ς2) receptor ligand, with a pKi of 8.02. -
Sigma-1 receptor antagonist
Sigma-1 receptor antagonist 3 (compound135) is a potent and selective Sigma-1 (??1) receptor antagonist with a Ki of 1.14 nM. -
sigma 1 receptor antagonist
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (??1 R) antagonist with Kis of 3.88 and 1288 nM for ??1 and ??2 receptor, respectively. -
Sigma receptor ligand
Sigma-LIGAND-1 is a selective sigma receptor ligand, has receptor IC50s of 16 nM at the DTG site, 19 nM at the PPP site, and a Ki of 4000 nM at the dopamine D2 receptor. -
5-HT2/sigma 2 receptor antagonist
Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia. -
Sigma-1 receptor agonist/muscarinic M1 agonist
Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand. -
sigma 1 receptor agonist
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(??1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4??1.9 nM); 100-fold less affinity for the sigma 2 receptor. -
Sigma receptor agonist
Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (??1/??2 receptor). - SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties.
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σ2 Receptor Agonist
PB28 dihydrochloride is a potent σ2 receptor agonist, exhibiting high affinity with a Ki of 0.68 nM, and also acts as a σ1 antagonist with a Ki of 0.38 nM. This compound demonstrates significant biological activity by inhibiting electrically evoked twitch responses in guinea pig bladder and ileum, with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride has been shown to modulate SARS-CoV-2-human protein-protein interactions, induce caspase-independent apoptosis, and display antitumor effects, making it a valuable tool for research in neuropharmacology and cancer biology. -
Sigma Receptor Agonist
CB-64D is a dual agonist of sigma receptor 1 and sigma receptor 2, exhibiting Ki values of 16.5 nM and 3063 nM, respectively. It has been shown to induce apoptosis in SK-N-SH cancer cells, highlighting its potential role in cancer research. This compound can serve as a valuable tool for investigating the biological functions of sigma receptors and their implications in various pathologies. -
Sigma Receptor Antagonist
BMY-14802 hydrochloride is a selective antagonist of the sigma receptor, exhibiting an IC50 of 112 nM. It also functions as an agonist for the 5-HT1A and adrenergic α1 receptors. BMY-14802 hydrochloride demonstrates antipsychotic activity, making it a valuable tool for research in neuropharmacology and the investigation of psychiatric disorders. -
Sigma Receptor Antagonist
NE-100 hydrochloride is a selective antagonist of the sigma-1 receptor, exhibiting an IC50 value of 4.16 nM. This compound demonstrates significant neuroprotective effects and has been shown to improve cognitive impairment, making it valuable in studies related to neurodegenerative disorders and psychiatric conditions. NE-100 hydrochloride is a useful tool for investigating the role of sigma receptors in the nervous system. -
σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
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.
