Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Sig1R PAM
(2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances cognitive and memory functions. This enantiomer of E1R is designed for research applications exploring the modulation of sigma-1 receptor activity, which has implications in treating cognition and memory disorders. Its selectivity and mechanism of action make it a valuable reagent in neuroscience studies. -
Sigma Receptor Antagonist
EST64454 maleate is a potent σ1 receptor antagonist, effectively demonstrating antinociceptive properties suitable for pain management research. With excellent metabolic stability in various species and a favorable pharmacokinetic profile in rodent models, EST64454 maleate stands out as a promising candidate for clinical applications. Its high aqueous solubility and suitable permeability through Caco-2 cell membranes further support its potential in drug development studies. -
Sigma Receptor
KSCM-5 is a high-affinity ligand for the sigma-1 receptor, exhibiting a Ki value of approximately 34 nM, which indicates significant selectivity. Its unique interaction with the sigma receptor makes KSCM-5 valuable for research applications in compound development targeting diseases related to sigma receptor dysregulation. This compound can provide insights into the therapeutic potential and mechanisms of sigma receptors in various biological processes. -
Sigma-1 Receptor Antagonist
Sigma-1 receptor antagonist 6 is a selective antagonist of the Sigma-1 receptor (σ1R), exhibiting significant antiallodynic properties. This compound effectively reduces mechanical allodynia in neuropathic pain models, particularly in response to paclitaxel treatment. Its application in research settings enables the exploration of σ1R modulation in pain pathways and the development of novel analgesic therapies. -
Cough Suppressant
Oxeladin is an orally active cough suppressant that functions as a selective sigma 1 receptor agonist with a Ki of 25 nM. This compound demonstrates significant potential in modulating cough reflex and can be utilized in research related to pulmonary diseases and stroke. Its ability to penetrate the blood-brain barrier further enhances its relevance in neuropharmacological studies. -
Sigma Receptor Modulator
(±)-PPCC hemioxalate is a selective modulator of the sigma-1 receptor, which plays a critical role in regulating intracellular calcium signaling between the endoplasmic reticulum and mitochondria. This compound promotes the dissociation of the sigma-1 receptor from the BIP complex, influencing cellular bioenergetics and survival. (±)-PPCC hemioxalate is suitable for research applications related to cocaine addiction, memory processes, pain modulation, depression, Alzheimer's disease, stroke, and cancer studies. -
Sigma Receptor Ligand
Sigma-LIGAND-1 hydrochloride is a selective ligand for sigma receptors, exhibiting IC50 values of 16 nM and 19 nM at the DTG and PPP sites, respectively. This compound demonstrates a Ki of 4000 nM at the dopamine D2 receptor, indicating its selectivity for sigma binding. It is valuable for research in neuropharmacology, particularly in studies exploring sigma receptor-mediated signaling pathways and their implications in various neurological disorders. -
Sig1R PAM
(Rac)-E1R is a racemic mixture that functions as a positive allosteric modulator of the sigma-1 receptor (Sig1R PAM). This compound has been investigated for its potential role in enhancing cognitive functions and memory processes. Research applications include the study of cognitive and memory disorders, making it a valuable tool in neuroscientific investigations. -
Sig1R PAM
(2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) that enhances receptor activity. This compound has demonstrated potential in the treatment of cognition and memory disorders by modulating signaling pathways associated with neuroprotection and cognitive enhancement. Its unique mechanism of action makes it a valuable tool for research in neurobiology and the development of therapies for neurodegenerative diseases. -
S1R Antagonist
PW507 is a selective antagonist of the sigma 1 receptor (S1R) with a binding affinity of Ki 7.5 nM for the human variant. With minimal interactions with the sigma 2 receptor (S2R) and hERG channel, PW507 is well-suited for studies requiring brain penetration. This compound is particularly relevant for investigating painful diabetic neuropathy (PDN) and other related conditions. -
Sigma Receptor Activator
CM764 is a sigma receptor activator, exhibiting Ki values of 86.6 nM for the sigma-1 receptor and 3.5 nM for the sigma-2 receptor. This compound increases cytoplasmic calcium levels, enhances NAD+/NADH and ATP production, and reduces reactive oxygen species (ROS) concentration. CM764 is relevant for studies exploring sigma receptor pathways and their implications in cellular metabolism and oxidative stress. -
Sigma Receptor Ligand
SAS-1121 is a selective ligand for the sigma 2 receptor and PGRMC1, exhibiting a Ki of 16.2 nM. It demonstrates a remarkable 574-fold selectivity for the sigma 2 receptor compared to the sigma 1 receptor. As a tertiary amine, SAS-1121 is valuable for studying mechanisms related to neurological conditions and offers potential insights into sigma receptor-related pathways in pharmacological research. -
Sig1R PAM
(2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM), specifically designed for enhancing cognitive function and memory. This enantiomer of E1R exhibits significant biological activity in modulating Sig1R, which is implicated in various neurological processes. Research applications include the investigation of cognitive and memory disorders, offering potential therapeutic insights for related conditions. -
Sigma (σ) Receptor Agonist
Opipramol dihydrochloride is a sigma (σ) receptor agonist that exhibits notable binding affinity, with a Ki value of 50 nM for sigma recognition sites. This atypical tricyclic antidepressant is primarily utilized in research related to generalized anxiety disorder (GAD). Opipramol's mechanism of action involves modulation of sigma receptor activity, highlighting its potential in elucidating the pathophysiology of anxiety disorders and evaluating novel therapeutic approaches. -
σ Receptor Ligand
E-5842 citrate is a selective σ receptor ligand with a Ki value of 4 nM for the σ1 receptor. This compound has been shown to enhance Fos protein levels in the medial prefrontal cortex and nucleus accumbens, while having no effect on protein levels in the striatum. E-5842 citrate is valuable for investigating the neurobiological mechanisms underlying psychiatric disorders. -
S1R Antagonist
AB21 is a potent and selective antagonist of the sigma-1 receptor (S1R), exhibiting an IC50 value of 13 nM for S1R with minimal activity against the sigma-2 receptor (S2R) at 102 nM. This compound is effective in reducing mechanical hypersensitivity, making it a valuable tool for research into pain modulation and related neurological disorders. Additionally, AB21 may facilitate studies into the role of S1R in various physiological and pathological processes. -
σ1 receptor Agonist
WLB-87848 is a selective σ1 receptor agonist with a Ki value of 9 nM, demonstrating high oral bioavailability and the ability to penetrate the blood-brain barrier. This compound has been shown to effectively rescue recognition memory impairment, making it a valuable tool for research in neurodegenerative diseases and memory-related disorders. Its specific targeting of the σ1 receptor positions WLB-87848 as a promising candidate for further investigation in cognitive enhancement studies. -
Sigma-1 Agonist
(±)-PPCC oxalate is a potent sigma-1 agonist, exhibiting high affinity for sigma-1 receptors with a Ki of 1.5 nM. It demonstrates significant anti-amnesic effects in rodent models of cognitive impairment, effectively enhancing cognitive function in both mild and severe cases. This compound is useful for research in neuropharmacology and the exploration of cognitive disorders. -
Sigma-2 Ligand
Sigma-2 Radioligand 1 is a selective ligand targeting the sigma-2 receptor. This radioligand demonstrates favorable biodistribution in murine models and exhibits significant in vivo activity in rat studies. Modified with [18F], Sigma-2 Radioligand 1 is suitable for micro-PET/CT imaging, displaying high tumor uptake and an optimal tumor-to-background ratio, particularly in U87MG glioma xenografts. Its specificity makes it a valuable tool for tumor visualization and research into sigma receptor biology. -
Sigma Receptors Antagonist
BD-1047 is a selective functional antagonist targeting sigma receptors. It demonstrates significant activity in modulating behaviors associated with dopamine signaling, reducing apomorphine-induced climbing and phencyclidine-induced head twitches. This compound is valuable for research applications in neuropharmacology and the study of sigma receptor biology. -
Sigma-2 Receptor Agonist
CM572 is a selective irreversible partial agonist of the sigma-2 receptor. It demonstrates significant antitumor activity, inducing dose-dependent cell death in SK-N-SH neuroblastoma cells, with an EC50 of 7.6 μM. This compound is valuable for researching various malignancies, including neuroblastoma and breast cancer. -
Sigma-1 Agonist
(±)-PPCC is a potent sigma-1 receptor agonist, exhibiting a binding affinity with a Ki value of 1.5 nM. This compound demonstrates significant anti-amnesic effects in both mild and severe cognitive impairment models in rats, leading to marked improvements in cognitive function. Its utility in neurological research makes it a valuable tool for studying the mechanisms underlying cognitive disorders and potential therapeutic interventions. -
Sigma-1 Receptor Ligand
KSCM-1 is a selective ligand for the sigma-1 receptor, exhibiting a Ki value of 27.5 nM. This compound demonstrates a marked selectivity for the sigma-1 receptor over sigma-2 receptors and exhibits minimal affinity for non-sigma receptor targets. KSCM-1 is valuable for studies investigating the role of sigma-1 receptors in various biological processes and neurological disorders. -
Antitussive Agent
Chlophedianol hydrochloride is a potent antitussive agent that acts primarily by suppressing the cough reflex in the central nervous system. This compound is useful in research focused on acute cough, particularly in the context of upper respiratory tract infections (URIs). Its efficacy in alleviating cough symptoms makes it a valuable tool for studies aimed at understanding cough mechanisms and developing new therapeutic strategies. -
Sigma-1 Receptor Allosteric Modulator
SOMCL-668 is a selective and potent allosteric modulator of the sigma-1 receptor. It has been demonstrated to enhance social interaction and alleviate cognitive impairments induced by the sigma-1 agonist PRE084. Additionally, SOMCL-668 exhibits anti-seizure properties, making it a valuable tool for research into psychotic illnesses and related neurological disorders. -
Sigma Receptor
Sigma-2 Radioligand 2 selectively targets the sigma-2 receptor with a low nanomolar affinity (Ki(σ2) = 2.30 nM) and exhibits significant subtype selectivity (Ki(σ1)/Ki(σ2) > 1500). This compound is essential for research applications involving sigma receptor pharmacology, allowing for in-depth studies of receptor function and potential therapeutic implications in neuropsychiatric disorders. -
σ1 Receptor Antagonist
σ1 Receptor Antagonist 4 is a selective antagonist targeting the sigma1 (σ1) receptor, exhibiting a Ki value of 10 nM. This compound shows weak activity at the sigma2 (σ2) receptor with a Ki of 370 nM and demonstrates no significant effects on dopamine (DAT), serotonin (SERT), or norepinephrine (NET) transporters. σ1 Receptor Antagonist 4 is primarily utilized in research to elucidate the role of the σ1 receptor in various biological processes and its potential implications in neurodegenerative diseases and psychiatric disorders. -
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. -
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. -
PROTAC Linker
2-[4-(Aminomethyl)triazol-1-yl]ethanamine is a specialized PROTAC linker that serves as a crucial component in targeted protein degradation strategies. This compound facilitates the synthesis of PROTAC CB1R Degrader-1, enabling the effective modulation of cannabinoid receptor 1 (CB1R) levels. Its application in research supports investigations into protein homeostasis and therapeutic approaches for various diseases. -
H3 Agonist
Immepip dihydrobromide acts as a selective agonist for the H3 histamine receptor. It is known to attenuate cortical histamine release, thereby influencing neurotransmitter dynamics. This compound is applicable in the study of neurological disorders, providing insights into histaminergic system modulation and its potential therapeutic effects. -
Smoothened Agonist
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist, with an EC50 of 3 nM and a Kd of 59 nM. This compound effectively activates the Hedgehog signaling pathway, providing a robust mechanism to counteract the inhibitory effects of Cyclopamine. SAG dihydrochloride is valuable for research in developmental biology, cancer biology, and therapeutic strategies targeting Hedgehog-related pathways. -
Smoothened Antagonist
KAAD-Cyclopamine is an antagonist of the Smoothened receptor, a critical component of the Hedgehog signaling pathway. This compound effectively inhibits hedgehog signaling, thereby influencing cell proliferation and differentiation processes. It is widely used in research related to developmental biology, cancer, and regenerative medicine, facilitating the study of signaling cascades and their implications in various diseases. -
hSMOX Inhibitor
JNJ-1289 is a potent and selective inhibitor of human spermine oxidase (hSMOX), exhibiting a competitive and allosteric mechanism of action with an IC50 value of 50 nM. This compound is primarily utilized in research studies focused on polyamine catabolism, inflammation, and various cancer models, providing valuable insights into the role of hSMOX in these biological processes. -
Smo Probe
BODIPY-Cyclopamine is a fluorescent ligand targeting the Smoothened (SMO) receptor, crucial for Hedgehog signaling pathway regulation. Dysregulation of this pathway is linked to tumorigenesis, making BODIPY-Cyclopamine valuable for research related to cancer biology. Utilizing the NanoBRET (Nanofluorescein bioluminescence resonance energy transfer) technique, this compound facilitates the sensitive detection of energy transfer between SMO and the fluorescent probe, enabling high-throughput screening and kinetic studies. Additionally, investigating the binding dynamics of BODIPY-Cyclopamine can assist in the development of SMO-targeted therapeutics. -
Smo Receptors Antagonist
MRT-81 is a potent antagonist of smoothened (Smo) receptors in both human and rodent models, exhibiting an IC50 value of 41 nM in Shh-light2 cells. This compound effectively inhibits hedgehog signaling pathways, making it a valuable tool in cancer research. Its ability to modulate Smo activity facilitates investigations into Hedgehog pathway-related tumors and their therapeutic interventions. -
Smo Antagonist
IHR-1 is a cell membrane impermeable antagonist of Smoothened (Smo), a key component of the Hedgehog signaling pathway. This compound effectively inhibits Smo activity, making it a valuable tool for studying Hedgehog-related biological processes and disease states, such as cancer and developmental disorders. IHR-1's specificity for Smo allows for targeted research into the mechanistic roles of this pathway in various cellular contexts. -
Smo Inhibitor
MRT-83 hydrochloride is a potent Smoothened (Smo) receptor antagonist. By inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo, MRT-83 hydrochloride demonstrates significant biological activity. This compound is particularly relevant for research applications focused on cancer and associated signaling pathways. -
Smo Antagonist
MRT-10 is a smoothened (Smo) antagonist that effectively inhibits Smo activity with an IC50 of 0.65 μM in various Hedgehog (Hh) signaling assays. By binding to the Bodipycyclopamine-binding site on the Smo receptor, MRT-10 serves as a valuable tool for investigating the roles of Hedgehog signaling in cancer biology. Its application may extend to studies focused on tumor growth and progression influenced by aberrant Hedgehog pathway activation. -
Smoothened Inhibitor
Glasdegib maleate is a potent smoothened inhibitor that selectively targets the human Smoothened (SMO) protein. With an IC50 value of 4 nM, this orally bioavailable compound effectively modulates the Hedgehog signaling pathway, making it valuable for research in cancer biology and developmental processes. Glasdegib maleate is primarily used in studies investigating tumor growth and metastasis driven by aberrant Hedgehog signaling. -
Smo Inhibitor
Glasdegib hydrochloride is a potent smoothened (SMO) inhibitor, primarily targeting the Hedgehog signaling pathway. It exhibits high affinity for human SMO, with an IC50 of 4 nM, making it an effective tool for research in cancer biology and developmental processes. This compound is valuable for studies investigating the role of SMO in tumorigenesis and therapeutic resistance in various malignancies.
