Catalog No.
Product Name
Application
Product Information
Citations
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p97 ATPase Inhibitor
p97-IN-2 is a selective inhibitor of the p97 ATPase, with an IC50 of 0.6 μM. This compound effectively inhibits the proliferation of cancer cell lines, including HCT15 (IC50 = 1.1 μM) and SW403 (IC50 = 0.8 μM). p97-IN-2 serves as a valuable tool for investigating the role of p97 in cancer biology and therapeutic applications. -
ERAD Inhibitor
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor that functions as a direct binder to VDAC1, VDAC2, and VDAC3. It demonstrates an IC50 of 1.02 μM for inhibiting ERAD and a Kd of 3.13 μM for binding human VDAC1. By disrupting cellular calcium homeostasis and enhancing VDAC1-IP3R coupling, NCATS-SM0225 activates the PERK pathway and selectively induces apoptosis in cancer cells. This reagent is valuable for investigating cancer biology, particularly in melanoma, as well as exploring the underlying mechanisms of ERAD and calcium homeostasis regulation. -
Serotonin And Norepinephrine Reuptake Inhibitor
Milnacipran is an orally active serotonin and norepinephrine reuptake inhibitor that primarily targets the monoamine transporters responsible for neurotransmitter reuptake. It demonstrates high affinity for the norepinephrine transporter and serotonin transporter, with Ki values of 31 nM and 8.5 nM, respectively. Milnacipran exhibits antidepressant, anxiolytic, and analgesic properties, and has been shown to inhibit pERK1/2 activation. This compound is applicable in the study of major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. -
Stable Isotope
Milnacipran-d5 hydrochloride is a deuterated form of Milnacipran hydrochloride, a potent serotonin and norepinephrine reuptake inhibitor. It targets monoamine transporters, exhibiting Ki values of 31 nM for the norepinephrine transporter and 8.5 nM for the serotonin transporter. With notable antidepressant, anxiolytic, and analgesic properties, Milnacipran-d5 hydrochloride is valuable for research on major depressive disorder, anxiety disorders, and neuropathic pain conditions such as fibromyalgia. Additionally, it has been shown to affect behavior in preclinical models, providing insights into its pharmacological mechanisms. -
Stable Isotope
Milnacipran-d10 hydrochloride is a deuterium-labeled form of the serotonin and norepinephrine reuptake inhibitor, Milnacipran hydrochloride. It effectively inhibits monoamine transporters, targeting the norepinephrine and serotonin transporters with reported Ki values of 31 nM and 8.5 nM, respectively. This compound exhibits antidepressant, anxiolytic, and analgesic properties, and has demonstrated efficacy in reducing biting behavior in murine models. Milnacipran-d10 hydrochloride is valuable for research applications focused on major depressive disorder, anxiety disorders, and neuropathic pain syndromes, such as fibromyalgia. -
RAD51 Inhibitor
DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications. -
Proton Pump Inhibitor
Ilaprazole sodium hydrate is a potent proton pump inhibitor that irreversibly targets H+/K+-ATPase, exhibiting an IC50 value of 6 μM in rabbit parietal cell preparations. This compound is primarily utilized in research related to gastric ulcers, providing insights into gastric acid secretion and its regulation. In addition, Ilaprazole sodium hydrate demonstrates inhibitory activity against TOPK (T-lymphokine-activated killer cell-originated protein kinase), making it a valuable tool for studies on cellular signaling pathways and cancer research. -
Calcium Influx/NO Modulator
Palmitoylglycine (N-palmitoyl glycine) is an endogenous lipid that functions as a modulator of calcium influx and nitric oxide production in sensory neurons. This compound is associated with an increased risk of Brugada syndrome (BrS) and interacts with various BrS-related proteins, displaying moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA. Palmitoylglycine is valuable in research investigating its roles in neuronal signaling and cardiovascular conditions linked to BrS. -
Calcium Channel Inhibitor
Ethacrynic acid sodium is an effective calcium channel inhibitor that primarily targets L-type voltage-dependent and store-operated calcium channels. This compound exhibits diuretic properties and significantly modulates glutathione S-transferases (GSTs) while inhibiting the NF-kB signaling pathway. Ethacrynic acid sodium demonstrates anti-inflammatory activity, evidenced by its ability to reduce retinoid-induced ear edema in murine models, making it a valuable tool in research focused on inflammation and airway smooth muscle relaxation. -
Calcium Channel Blockers
Levamlodipine hydrochloride is a dihydropyridine calcium channel blocker that primarily targets L-type calcium channels on vascular smooth muscle cells. By inhibiting calcium ion influx, it promotes vasodilation, effectively lowering blood pressure and alleviating angina. Additionally, its binding affinity to human serum albumin (HSA) enhances research into drug transport and release mechanisms within the body. This compound is beneficial for studies focused on cardiovascular therapies and mechanisms of action related to hypertension and coronary artery disease. -
Calcium Channel Inhibitor
Levamlodipine hydrobromide is a calcium channel inhibitor with notable antioxidant and vasodilatory properties. This compound has been shown to reduce serum malondialdehyde (MDA) levels while increasing superoxide dismutase (SOD) activity, thus improving oxidative stress responses. It is appropriate for research applications related to vascular dementia, hypertension, and cerebrovascular diseases. -
Calcium Channel Blocker
Levamlodipine besylate hemipentahydrate is a calcium channel blocker that exhibits significant antioxidant and vasodilatory effects. This compound has been shown to lower serum malondialdehyde (MDA) levels while enhancing superoxide dismutase (SOD) activity, thereby mitigating oxidative stress. Levamlodipine besylate hemipentahydrate is suitable for research applications focused on vascular dementia, hypertension, and cerebrovascular diseases. -
TLR4/HCN Inhibitor
HCN-IN-1 is a TLR4 inhibitor and modulator of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, specifically targeting HCN2 and HCN4. It effectively inhibits TLR4-mediated signaling, evidenced by reduced alkaline phosphatase activity. HCN-IN-1 modulates HCN2 currents by shifting the voltage-dependent activation to hyperpolarized potentials and slowing activation kinetics, while also blocking currents through HCN4 channels. This compound demonstrates significant analgesic, anti-inflammatory, and anti-anginal properties, making it valuable for research into inflammatory pain, neuropathic pain, heart failure, and related inflammatory conditions. -
Calcium Antagonist
F-0401 is a calcium antagonist that exerts its effects through antagonism of the platelet-activating factor receptor (PAFR). This compound demonstrates significant potential in neurological research, particularly in studies related to stroke and related pathologies. Its ability to modulate calcium signaling pathways makes F-0401 a valuable tool for investigating therapeutic strategies in the context of neuroprotection and cerebrovascular disorders. -
δ2-opioid Receptor Antagonist/TRPM7 Activator
Naltriben mesylate is a potent antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It demonstrates high affinity, with Ki values of 0.013 nM for the δ receptor, alongside 19 nM and 152 nM for μ and κ receptors, respectively. Research indicates that Naltriben mesylate enhances glioblastoma cell migration and invasion, making it a valuable tool for studies related to neurological diseases and cancer biology. -
μ-opioid Receptor Activator, hERG (Kv11.1) Potassium Channel Inhibitor
ERG-IN-6 is a potent μ-opioid receptor activator, exhibiting an EC50 of 0.12 nM, which makes it an effective tool for studies related to pain modulation. Additionally, ERG-IN-6 functions as a hERG (Kv11.1) potassium channel inhibitor with an IC50 of 0.681 μM. This compound is valuable for research applications investigating the interplay between opioid signaling and ion channel regulation. -
ORL1 Receptor Antagonist
MK-1925 is a selective ORL1 receptor antagonist, demonstrating human IC50 values of 8.2 nM and 4.6 nM. This compound exhibits oral bioavailability and the capability to penetrate the blood-brain barrier, making it a valuable tool for neuroscience research. MK-1925 specifically inhibits the ORL1 receptor without significant interaction with other opioid receptors or the hERG potassium channel, positioning it as a potential candidate for studies focused on pain modulation and opioid receptor mechanisms. -
ORL1 Antagonist
ORL1 antagonist 2 is a selective antagonist of the opioid receptor-like 1 (ORL1). This compound has been primarily utilized in the study of P-glycoprotein (P-gp) interactions and transport mechanisms. Its ability to modulate ORL1 activity makes it a valuable tool in research aimed at understanding opioid signaling pathways and their implications in various physiological and pathological processes. -
Na+ Channel Blocker
RSD-921 is a potent sodium (Na+) channel blocker exhibiting significant anti-arrhythmic properties. It acts with state- and voltage-dependent inhibition on the open states of cardiac, skeletal muscle, and neuronal Na+ channels. Additionally, RSD-921 has a low affinity for κ-opioid receptors and shows weak κ-agonistic activity in vitro. This reagent is valuable for research focusing on cardiac arrhythmias and the modulation of Na+ channels in various biological models. -
TRPV1 Antagonist/MOR Agonist
TRPV1 Antagonist 11 is a potent antagonist of the TRPV1 receptor, exhibiting an IC50 of 29.3 nM. Additionally, it serves as a μ-opioid receptor (MOR) agonist with a Ki value of 60.3 nM. This compound demonstrates significant analgesic properties by antagonizing TRPV1, thereby reducing pain signaling, and activating MOR, which enhances the pain-relief effect. TRPV1 Antagonist 11 has been shown to provide a robust, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice, making it a valuable tool for pain research. -
δ2-opioid Receptor Antagonist/TRPM7 Activator
Naltriben is a selective antagonist of the δ2-opioid receptor and an activator of TRPM7 channels. It has been shown to enhance migration and invasion of glioblastoma cells, making it a valuable tool for studying tumor biology. This compound is suited for research into neurological disorders and cancer mechanisms, providing insights into therapeutic approaches targeting these areas. -
OT Receptor Agonist
(Thr4,Gly7)-Oxytocin is a specific agonist of the oxytocin receptor (OT receptor). This analogue enhances neuronal excitability in subicular neurons through the activation of TRPV1 channels and the inhibition of K+ channels. Its unique properties make it valuable for research applications involving neurobiology and the study of oxytocin-related pathways. -
TRPV1 Inhibitor
(±)-Eriodictyol is a potent TRPV1 receptor antagonist, exhibiting an IC50 value of 44-47 nM in rTRPV1 assays. This compound demonstrates significant antioxidant and anti-inflammatory properties, effectively inhibiting lipid peroxidation and reducing the release of proinflammatory cytokines. By modulating the Nrf2 signaling pathway, (±)-Eriodictyol helps maintain the integrity of the blood-retinal barrier and can alleviate oxidative stress-induced apoptosis and hyperalgesia. It has potential applications in the research of diabetic retinopathy, acute lung injury, and various pain-related conditions, while also enhancing immune cell activity and promoting antioxidant enzyme levels. -
Histamine H1 Receptor Antagonist
Terfenadine N-oxide is a histamine H1 receptor antagonist with an IC50 value of 2.73 μM, also exhibiting inhibition of the hERG potassium channel with an IC50 of 0.698 μM. This compound is valuable for investigating histamine-related allergic diseases and the role of hERG channels in arrhythmias. Its dual activity makes it a useful tool for research in pharmacology and toxicology related to allergic responses and cardiac rhythm disturbances. -
Antispasmodic Agent
Terodiline is an antispasmodic agent that primarily targets the hERG potassium channel, exhibiting an IC50 of 375 nM. It possesses both anticholinergic and calcium antagonist properties, making it effective in reducing abnormal bladder contractions associated with detrusor instability. Terodiline is suitable for research applications focused on urinary incontinence. -
Calcium Channel
C18 LPA (PA(18:0e/0:0)) targets calcium channels and serves as a bioactive phospholipid involved in signal transduction via G protein-coupled receptors (GPCRs). This compound promotes smooth muscle contraction, chemotaxis, cytoskeletal rearrangement, and is implicated in neurotransmitter release and cell proliferation. Increased levels of C18 LPA in human plasma are correlated with ovarian cancer and atherosclerosis, indicating its potential utility as a biomarker in oncological and cardiovascular research. -
HCN Channel Blocker
Ivabradine impurity 1 is a derivative of Ivabradine, a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. This compound has been utilized in research to investigate the modulation of cardiac rhythms and treatment of conditions such as angina and heart failure. Its biological activity contributes to the understanding of ion channel interactions and cardiac electrophysiology. -
Overoxidized By-product of Lansoprazole
Lansoprazole N-oxide is the overoxidized by-product derived from the synthesis of the proton pump inhibitor Lansoprazole. This compound is of interest for studies related to gastrointestinal disorders, including duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Researchers may utilize Lansoprazole N-oxide to deepen the understanding of proton pump inhibition and its implications in these conditions. -
Drug Metabolite
15-Hydroxy Lubiprostone is an active metabolite of the laxative drug Lubiprostone, primarily targeting chloride channels. This compound exhibits biological activity by promoting fluid secretion in the intestinal lumen, thereby facilitating bowel movements. It is mainly utilized in research applications focused on gastrointestinal pharmacology and the mechanisms of action related to chloride channel activation. -
Overoxidized By-product of Lansoprazole
Lansoprazole sulfone N-Oxide is an overoxidized by-product generated during the synthesis of the proton pump inhibitor Lansoprazole. This compound is relevant for research into gastrointestinal conditions, such as duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Its study may provide insights into the metabolic pathways and potential therapeutic implications related to proton pump inhibition. -
Bupivacaine metabolite
Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives. -
Active Metabolite of T-1095
T-1095A is the active metabolite of T-1095, functioning as a sodium-glucose cotransporter (SGLT) inhibitor. This compound demonstrates significant biological activity in the regulation of glucose reabsorption in the renal system and is primarily utilized in research related to diabetes and metabolic disorders. Its mechanism of action aids in the investigation of glucose homeostasis and associated therapeutic strategies. -
Sodium Channel Inhibitor
Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology. -
Drug Metabolite Control
Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems. -
EBP Inhibitor
EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders. -
Vitamin E
γ-Tocotrienol is an active form of vitamin E that primarily targets the signaling pathway of NF-κB and P-glycoprotein (P-gp). It demonstrates significant biological activity by reversing multidrug resistance (MDR) in breast cancer cells, enhancing the efficacy of chemotherapeutic agents. Additionally, γ-tocotrienol serves as a radioprotective agent, effectively mitigating bone marrow radiation damage associated with targeted radionuclide treatments. Research applications include cancer therapy and protection against radiation-induced injury. -
Active Metabolite
Desacetyl bisacodyl is the active metabolite of the laxative bisacodyl, primarily targeting epithelial chloride channels. This compound is known to stimulate chloride secretion in the colon and rectum of rat models, leading to increased mucus and electrolyte secretion. It is utilized in research applications focused on gastrointestinal physiology and the mechanisms underlying laxative action. -
Tricyclic Antidepressant Trimipramine Active Metabolite
Trimipramine N-oxide is the active metabolite of the tricyclic antidepressant trimipramine, primarily targeting human monoamine transporters. It effectively inhibits noradrenaline (hNAT), serotonin (hSERT), and dopamine (hDAT) transporters, along with human organic cation transporters (hOCT1 and hOCT2), with IC50 values of 11.7, 3.59, 9.4, 9.35, and 27.4 nM, respectively. This compound is valuable for research focused on depression and anxiety, contributing to the understanding of mood disorders and the pharmacological mechanisms of antidepressants. -
ATPase
Creatine phosphokinase, Rabbit muscle (CPK) is an enzyme that catalyzes the reversible conversion of creatine and ATP into phosphocreatine and ADP. By facilitating the maintenance of an optimal ATP/ADP ratio, CPK plays a critical role in energy metabolism, particularly during periods of high energy demand. This enzyme is widely used in biochemical research to study cellular energy dynamics and various metabolic disorders. -
BCRP Inhibitor
5,7-Dimethoxyflavone is a potent inhibitor of the Breast Cancer Resistance Protein (BCRP). It exhibits significant biological activities, including anti-obesity, anti-inflammatory, and antineoplastic effects. Additionally, this compound has been shown to inhibit cytochrome P450 (CYP) 3A enzymes, making it valuable for research applications focused on drug resistance and metabolic pathways in cancer therapy. -
Sodium Channel Blocker
CAY10568 is a sodium channel blocker that modulates neuronal excitability. This compound, a derivative of QX-314, exhibits a smaller and less hydrophobic profile, making it suitable for exploring its effects on inflammation and pain perception. CAY10568 is valuable for research applications aimed at understanding pain mechanisms and developing analgesic therapies. -
Sodium Channel Inhibitor
(-)-Sparteine sulfate pentahydrate is a sodium channel inhibitor that acts as a class 1a antiarrhythmic agent. It has demonstrated notable biological activity in modulating cardiac excitability and can be utilized in research focusing on arrhythmias and pharmacological studies related to ion channel function. This reagent is suitable for investigating the effects of sodium channel blockade in various biological models. -
Nav1.7 Inhibitor
Nav1.7-IN-6 is a selective inhibitor targeting the voltage-gated sodium channel Nav1.7, which is important in pain signaling pathways. This compound demonstrates significant biological activity in modulating neuronal excitability, making it a valuable tool for research on pain mechanisms and potential therapeutic interventions in pain disorders. Its specificity for Nav1.7 enhances its utility in elucidating the role of this channel in nociception and related studies. -
NaV1.7 Antagonist
AMG8379 is a selective sulfonamide antagonist targeting the voltage-gated sodium channel NaV1.7. It demonstrates potent inhibition with IC50 values of 8.5 nM for human NaV1.7 and 18.6 nM for mouse NaV1.7, effectively blocking TTX-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM. This compound is useful for research applications related to pain pathways and sodium channel modulation. -
Sodium Channel Inhibitor
B-GYKI-38233 hydrochloride is a sodium channel inhibitor that exhibits potent antiarrhythmic properties. This compound is utilized in research focused on the modulation of sodium channels, which play a critical role in cardiac excitability and conductivity. Its mechanism of action makes it a valuable tool for the investigation of arrhythmias and related cardiovascular disorders. -
Nav1.8 channel Inhibitor
Nav1.8-IN-10 is a selective inhibitor of the Nav1.8 ion channel. At a concentration of 4 nM, it achieves an impressive blocking rate of 79.4%, demonstrating its potency. This compound is primarily utilized in the research of pain disorders, facilitating investigations into the modulation of pain pathways and potential therapeutic interventions. -
Nav1.8 Inhibitor
Nav1.8-IN-5 is a selective inhibitor of the voltage-gated sodium channel Nav1.8. It demonstrates potent biological activity against Nav1.8-mediated pain and pain-related disorders, making it a valuable tool for research in these areas. Additionally, Nav1.8-IN-5 can facilitate studies related to cardiovascular diseases, including conditions such as atrial fibrillation, by modulating sodium channel activity. -
Sodium Channel Inhibitor
R 59494 is a sodium channel inhibitor that effectively blocks Na+ and Ca2+ uptake triggered by veratridine exposure. This compound exhibits significant anti-ischemic properties, making it valuable for research in cardiovascular and neuroprotective studies. Its ability to modulate ion channel activity positions R 59494 as a useful tool for investigating the mechanisms of ischemia-related cellular damage. -
Nav1.7 Blocker
NAV 26 is a selective blocker of the voltage-gated sodium channel Nav1.7, exhibiting an IC50 of 0.37 μM. This compound is valuable for investigating pain mechanisms and developing novel analgesics. Its specificity for Nav1.7 makes it a crucial tool in researching pain pathways and potential therapeutic interventions. -
NaV1.8 Channel Inhibitor
Analgesic agent-2 is a selective NaV1.8 channel inhibitor, exhibiting a reported IC50 of 50.18 nM in HEK293 cells expressing the human NaV1.8 channel. It demonstrates significant analgesic activity, making it a valuable tool for pain research. This compound is ideal for studies investigating the role of NaV1.8 in nociception and the development of novel analgesic therapies.
