Catalog No.
Product Name
Application
Product Information
Citations
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TRPV4 Agonist
4α-Phorbol 12,13-didecanoate is a potent agonist of the transient receptor potential vanilloid 4 (TRPV4). It facilitates calcium ion influx and induces ATP release, thereby serving a role as an osmoreceptor. In animal studies, 4α-Phorbol 12,13-didecanoate has been shown to inhibit water intake and elevate maximal micturition pressure in rats. This compound is valuable for research into inflammation, infection, and the biological mechanisms underlying conditions such as chikungunya virus (CHIKV). -
TRPML Agonist
ML-SA1 is a selective agonist of TRPML channels, promoting lysosomal acidification and enhancing protease activity, which leads to the inhibition of Dengue virus 2 (DENV2) and Zika virus (ZIKV). The compound exhibits IC50 values of 8.3 μM for DENV2 RNA and 52.99 μM for ZIKV RNA. Additionally, ML-SA1 stimulates autophagy, making it a valuable tool for research into broad-spectrum antiviral strategies. -
Anti-malarial Agent
Quinine sulfate hydrate (2:1:4) is an orally active alkaloid used primarily as an anti-malarial agent. This compound functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM observed in response to voltage pulses of +100 mV. It is valuable for research applications focused on malaria treatment and investigating ion channel physiology. -
Anti-malaria Agent
Quinine hydrochloride is an alkaloid extracted from the bark of the cinchona tree, primarily functioning as an anti-malarial agent. It acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel and demonstrating inhibitory effects on channel currents evoked by voltage pulses to +100 mV, with an IC50 value of 169 μM. This compound is widely utilized in research applications related to malaria treatment and ion channel studies. -
Anti-malarial Agent
Quinine hemisulfate is an orally active alkaloid derived from cinchona bark, primarily recognized for its anti-malarial properties. This compound acts as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 value of 169 μM for channel currents induced by voltage pulses to +100 mV. Quinine hemisulfate serves as a valuable reagent for anti-malarial studies and relevant pharmacological investigations. -
Anti-malarial Agent
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark, primarily used as an anti-malarial agent. It functions as a potassium channel inhibitor, specifically targeting the WT mouse Slo3 (KCa5.1) channel, with an IC50 of 169 μM. This compound is utilized in various research applications aimed at understanding malaria pathophysiology and exploring therapeutic strategies for its treatment. -
Stable Isotope
Quinine-d3 is a deuterium-labeled derivative of quinine, primarily used as a stable isotope in chemical research. Quinine is an alkaloid isolated from the cinchona tree, known for its efficacy as an antimalarial agent and its role as a potassium channel inhibitor. It specifically inhibits wild-type mouse Slo3 (KCa5.1) channel currents induced by voltage pulses, exhibiting an IC50 of 169 μM. This reagent facilitates studies in pharmacology and biochemistry, enabling precise tracking and quantification in various applications. -
CV-B3 2C ATPase Inhibitor
ATPase-IN-8 is a selective inhibitor of CV-B3 2C ATPase, exhibiting an IC50 of 1.4 μM. This compound demonstrates significant anti-enteroviral activity, particularly against coxsackievirus B3 (CV-B3) and enterovirus D68 (EV-D68). ATPase-IN-8 is suitable for research applications focusing on enteroviral infections and their molecular mechanisms. -
Adenosine Receptor Antagonist
Swertisin is an adenosine A1 receptor antagonist with additional SGLT2 inhibitory activity. This compound exhibits various biological functions, including anti-diabetic and antioxidant properties, as well as the ability to inhibit hepatitis B virus (HBV). Research has demonstrated that Swertisin can enhance cognitive function and alleviate memory impairments in murine models, making it a valuable tool for studies in diabetes, neuroprotection, and viral infections. -
H+, K+-ATPase Inhibitor
Esomeprazole magnesium salt is a selective inhibitor of the H+, K+-ATPase enzyme in gastric parietal cells, functioning as an effective proton pump inhibitor. This compound demonstrates significant biological activity by reducing gastric acid secretion. It is primarily utilized in research related to gastroesophageal reflux disease, exploring its therapeutic potential and mechanisms of action in acid-related disorders. -
Proton Pump Inhibitor
S-Pantoprazole sodium trihydrate is a potent proton pump inhibitor that effectively reduces gastric acid secretion. It is primarily utilized in the treatment of conditions associated with excessive gastric acid production, such as gastroesophageal reflux disease (GERD) and peptic ulcers. Its mechanism of action involves the irreversible inhibition of the H+/K+ ATPase enzyme in gastric parietal cells, providing therapeutic benefits in managing acid-related disorders. -
Na+-V-ATPase Inhibitor
V-161 is an orally active inhibitor of Na+-V-ATPase, exhibiting an IC50 of 144 nM. This compound effectively inhibits the growth of Enterococcus hirae and Vancomycin-resistant Enterococcus faecium (VRE) under alkaline conditions, with a minimum inhibitory concentration (MIC) of 4 µg/mL for both bacterial strains. In vivo studies demonstrate that V-161 significantly reduces VRE colonization in the mouse small intestine, making it a valuable tool for research into antimicrobial resistance and gut microbiota interactions. -
Proton Pump Inhibitor
Lansoprazole sulfide-d4 is a deuterium-labeled form of Lansoprazole sulfide, a bioactive metabolite of the proton pump inhibitor Lansoprazole. This compound exhibits significant activity against Mycobacterium tuberculosis, demonstrating IC50 values of 0.59 μM intracellularly and 0.46 μM in broth. It is a valuable tool for research into anti-tubercular therapies and the pharmacokinetics of proton pump inhibitors. -
CCR5 Antagonist
AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis. -
CCR8 Antagonist
AZ760 is a potent antagonist of the CCR8 receptor, which plays a significant role in immune response modulation. This compound demonstrates excellent potency and favorable lipophilicity, resulting in a high free fraction in blood. However, it is important to note that AZ760 exhibits unacceptable inhibition of the hERG potassium channel, which may have implications for cardiovascular safety in therapeutic applications. -
CGRP/TRPV1 Inhibitor
Chrysin 6-C-glucoside 8-C-arabinoside is a potent inhibitor of calcitonin gene-related peptide (CGRP) release and the TRPV1 channel activation. This compound exhibits significant biological activity relevant to nociceptive signaling pathways, making it a valuable tool for anti-migraine research. Its mechanism of action offers insights into potential therapeutic strategies for migraine and related pain disorders. -
OCT1 Inhibitor
Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) selectively inhibits the organic cation transporter OCT1, with an IC50 value of 6.6 μM. This compound also acts as a competitive inhibitor of tyrosine hydroxylase, reducing dopamine biosynthesis with an IC50 of 20.7 μM in PC12 cells. Hydrastine is particularly relevant for research into Parkinson's disease, as it may induce neuronal toxicity through mitochondrial dysfunction and has the potential to exacerbate apoptosis when used in conjunction with L-DOPA. -
Fatty Acid Dopamide
N-Palmitoyl dopamine is a long-chain fatty acid dopamide that interacts with endovaniloids, exhibiting 'entourage' effects on N-arachidonoyl-dopamine (NADA) and anandamide. This compound is not active on the TRPV1 receptor, highlighting its selective profile. N-Palmitoyl dopamine is valuable for research applications focused on cannabinoid and pain signaling pathways, particularly in studies examining the interplay between fatty acid derivatives and endocannabinoid activity. -
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. -
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. -
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. -
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. -
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. -
TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM.
