Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Endogenous Metabolite
9(R)-HODE is a monohydroxy fatty acid and an endogenous metabolite of linoleic acid, generated through the enzymatic actions of cyclooxygenase (COX) and lipoxygenase (LO). This compound is known to promote chemotaxis and elevate the expression of chemokine receptors CCR9 and CXCR4 in immune cells. Additionally, 9(R)-HODE effectively inhibits interleukin-6 (IL-6) release in primary human monocytes and suppresses CD3α- and CD28-induced proliferation in isolated human peripheral blood lymphocytes at a concentration of 25 μg/mL, making it a valuable tool for studying immune responses and inflammatory processes. -
2-arachidonoylglycerol derivative
1-Monoarachidin is a 2-arachidonoylglycerol derivative that primarily acts as a modulator of cannabinoid receptors. This fatty acid plays a crucial role in the endocannabinoid system, contributing to various biological processes such as inflammation and neuroprotection. It is utilized in research to investigate the physiological effects of endocannabinoids and their potential therapeutic applications in neurological and inflammatory disorders. -
O-Alkyl-N-acyloxy Homologues
Oxy-Arachidonoyl ethanolamide is an O-alkyl-N-acyl oxime derivative that acts on O-Alkyl-N-acyl homologues. This compound exhibits significant biological activity, particularly in the modulation of endocannabinoid systems. It is employed in research applications focusing on cannabinoid receptor signaling, lipid metabolism, and neuroprotective studies, illuminating potential therapeutic pathways for various neurological diseases. -
Endogenous Metabolite
N-Methylarachidonamide is an analog of the endogenous cannabinoid anandamide, primarily targeting the central cannabinoid receptor (CB1). This compound exhibits a binding affinity with a Ki value of 60 nM for CB1, influencing various physiological processes. Additionally, it effectively inhibits rat glial gap junction cell-cell communication by 100% at a concentration of 50 μM. As such, N-Methylarachidonamide is a valuable tool for research exploring cannabinoid receptor signaling and its implications in neurobiology and related fields. -
FAAH Inhibitor
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone is a potent inhibitor of fatty acid amide hydrolase (FAAH) with a pI50 of 5.89. This compound exhibits significant activity against endocannabinoids and lipid mediators, making it relevant for studies in pain management, inflammation, and cannabinoid signaling pathways. Its limited affinity for cannabinoid receptors CB(1) and CB(2) allows for targeted research into FAAH-related physiological processes without direct receptor modulation. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Endothelin Receptor Antagonist
Edonentan is a potent endothelin receptor antagonist, specifically targeting the ETA receptor with an affinity (Ki) of 10 pM. This compound demonstrates metabolic stability and favorable pharmacokinetic properties in rat models. Edonentan effectively modulates the endothelin system by inhibiting the hypertensive response induced by big endothelin, making it a valuable tool for research in cardiovascular and renal disease studies. -
Endothelin Receptor Antagonist
PD 145065 is a highly potent non-selective endothelin receptor antagonist, demonstrating an IC50 value of 4 nM for the ETA receptor in rabbit renal artery vascular smooth muscle cells. This compound effectively inhibits endothelin signaling, making it useful for investigating the role of endothelin in cardiovascular biology and related disorders. PD 145065 is a valuable tool for researchers studying vascular physiology and potential therapeutic interventions targeting endothelial dysfunction. -
ETA Receptor Antagonist
SB234551 is a selective antagonist of the endothelin ETA receptor, inhibiting its activity to study its physiological effects. This compound has demonstrated potential in investigations related to stroke models, providing valuable insights into the role of endothelin in cerebrovascular events. Its selective targeting facilitates research into therapeutic strategies for conditions associated with altered endothelin signaling. -
ETB Receptor Agonist
Endothelin (16-21) functions as a selective agonist for the ETB receptor, exhibiting an EC50 of 228 nM in guinea-pig bronchus. This compound effectively induces smooth muscle contraction, making it a valuable tool for studying respiratory conditions such as asthma and cardiovascular diseases, including hypertension. Its targeted mechanism provides insights into ETB receptor signaling pathways relevant to these medical research applications. -
Vasoconstrictor
Big Endothelin-1 (22-38), human is a fragment of the human Big Endothelin-1 propeptide, specifically the 22-38 amino acid sequence. This peptide plays a crucial role in the regulation of vascular tone as it serves as a precursor to the potent vasoconstrictor Endothelin-1. It is utilized in research to study vascular physiology, hypertension, and related cardiovascular disorders, offering insights into the mechanisms of vasoconstriction and its effects on blood pressure regulation. -
Vasodilator
CH-141 is a peripheral vasodilator that acts to dilate blood vessels, thereby reducing vascular resistance. It is primarily employed in hypertension research to investigate mechanisms of blood pressure regulation and vascular function. This compound is instrumental in studying therapeutic strategies for cardiovascular diseases. -
ET Receptor Antagonist
A-127722 is a selective antagonist of the endothelin A (ETA) receptor, functioning through inhibition of endothelin signaling pathways. It exhibits a potent IC50 value of 0.36 nM, making it a valuable tool for research into cardiovascular diseases and conditions associated with endothelin dysregulation. This compound is particularly useful for studies investigating the role of endothelin in hypertension, heart failure, and pulmonary arterial hypertension. -
ETA/ETB Receptor Antagonist
L-749329 is a potent antagonist of the endothelin receptor subtypes ETA and ETB, exhibiting binding affinities (Kis) of 0.062 nM and 2.25 nM, respectively. This compound effectively inhibits endothelin-1 (ET-1)-stimulated signaling pathways, making it a valuable tool for studying the role of endothelin receptors in pathophysiological conditions. L-749329 is applicable in research focused on cardiovascular diseases, vascular biology, and related fields where endothelin signaling is implicated. -
Endothelin Receptor Antagonist
Atrasentan sodium is a selective endothelin receptor antagonist, exhibiting an IC50 of 0.0551 nM for the ETA receptor. This compound demonstrates significant biological activity by inhibiting endothelin-1-mediated vasoconstriction and fibrosis. Atrasentan sodium is primarily utilized in research applications related to cardiovascular diseases, pulmonary hypertension, and kidney injury, making it valuable for studies on endothelin signaling pathways and potential therapeutic interventions. -
ET Receptor Antagonist
Aselacin B is an endothelin-1 receptor antagonist that inhibits the binding of endothelin-1 to both ETA and ETB receptors. This compound plays a significant role in the investigation of cardiovascular diseases by modulating endothelin signaling pathways. Its application may provide insights into the pathophysiology of conditions such as hypertension and heart failure. -
ETA Receptor Antagonist
FR139317 is a selective antagonist of the endothelin A (ETA) receptor. This compound effectively inhibits cerebral activation induced by endothelin-1 in conscious rat models. Additionally, FR139317 demonstrates the capability to reduce cerebral vasospasm in canine subjects, highlighting its relevance in studies related to vascular regulation and cerebrovascular conditions. -
Endothelin Receptor Antagonist
WS009B is a selective endothelin receptor antagonist, exhibiting IC50 values of 0.67 μM for ET-1 and 0.8 μM for ET-2. This compound is useful for research into cardiovascular diseases, as it modulates the endothelin signaling pathway, which plays a critical role in vascular homeostasis and pathological conditions. WS009B's antagonistic properties make it a valuable tool for elucidating the mechanisms underlying endothelin-mediated physiological and pathological processes. -
ET(A)/ET(B) Antagonist
ATZ-1993 is a potent orally active nonpeptide antagonist of endothelin receptor subtype A and B, exhibiting pKi values of 8.69 and 7.20, respectively. This compound demonstrates significant potential in the study of intimal hyperplasia following balloon denudation of the carotid artery. ATZ-1993 can serve as a valuable tool in cardiovascular research, aiding in the exploration of vascular remodeling and related pathophysiological processes. -
Endothelin Receptor Antagonist
BMS 182874 hydrochloride is a highly selective antagonist of the endothelin ETA receptor, exhibiting an IC50 value of 0.150 μM and a Ki of 0.055 μM. This compound demonstrates efficacy in reducing arterial pressure in rat models of hypertension induced by deoxycorticosterone acetate. BMS 182874 hydrochloride is suitable for research applications focused on cardiovascular diseases and endothelin receptor modulation. -
Endothelin B Receptor Antagonist
IRL 1038 is a selective antagonist for the endothelin B receptor, with a binding affinity characterized by a Ki range of 6-11 nM. This compound effectively inhibits the actions of endothelin-1, crucial for studies investigating vascular function, cardiovascular diseases, and related physiological processes. Its application is valuable in elucidating the role of endothelin signaling in various pathophysiological conditions. -
ETA/ETB Receptor Antagonist
IRL-3630 is a selective antagonist of the ETA and ETB receptors, exhibiting binding affinities with Ki values of 1.9 nM and 1.2 nM, respectively. This compound is instrumental in studying the role of endothelin receptors in various physiological and pathological processes. Its applications include cardiovascular research, pulmonary hypertension studies, and investigations into renal function. -
ETA Receptor Antagonist
Clazosentan disodium is a selective endothelin A (ETA) receptor antagonist that effectively inhibits ET-1-mediated vasoconstriction. This compound is utilized in research focused on preventing cerebral vasospasm and related cerebral infarction. Its application may be significant in studies concerning vascular response and associated neurological conditions.
