Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
Tolbutamide-d9 is a deuterated form of Tolbutamide, which primarily targets ATP-sensitive potassium channels. As a first-generation sulfonylurea, it functions as an oral hypoglycemic agent, playing a critical role in glucose regulation. This stable isotope is valuable for metabolic research and isotopic tracing studies, facilitating investigations into pharmacokinetics and the mechanism of action of sulfonylureas. -
CFTR Inhibitor
BPO-27 racemate is a potent cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor, exhibiting an IC50 of 8 nM. This compound has been shown to effectively suppress CFTR activity, making it valuable for research aimed at understanding CFTR-related disorders. BPO-27 racemate can be utilized in studies investigating ion channel regulation and potential therapeutic interventions for cystic fibrosis. -
Stable Isotope
Omeprazole-d3 is a deuterium-labeled variant of Omeprazole, a widely used proton pump inhibitor (PPI) targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) between 2 to 6 μM, and has been shown to inhibit the growth of both Gram-positive and Gram-negative bacteria. This stable isotope is particularly useful for pharmacokinetic studies, metabolic profiling, and investigations into drug-drug interactions involving Omeprazole. -
Stable Isotope
Omeprazole-13C,d3 is a stable isotope-labeled form of Omeprazole, a proton pump inhibitor (PPI) that targets gastric acid secretion. This compound is utilized in pharmacokinetic studies due to its competitive inhibition of CYP2C19 activity, with an inhibition constant (Ki) ranging from 2 to 6 μM. Additionally, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome release. It is a valuable reagent for research in gastrointestinal physiology, drug metabolism, and cellular signaling pathways. -
CFTR Corrector
Tezacaftor-d4 is a deuterium-labeled CFTR corrector that targets the F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. By facilitating the proper trafficking of CFTR to the cell surface, Tezacaftor-d4 enhances functional chloride transport in epithelial cells. This compound is primarily utilized in research focused on developing therapeutic strategies for cystic fibrosis by restoring CFTR activity. -
Stable Isotope
Reserpine-d9 is a deuterated form of Reserpine that serves as an inhibitor of the vesicular monoamine transporter 2 (VMAT2). This stable isotope-labeled compound is valuable for studies in neuropharmacology and metabolism, allowing for precise tracking and quantification of Reserpine interactions in various biological systems. It enables researchers to explore its effects on neurotransmitter release and potential applications in psychiatric and neurological disorders. -
Autophagy Inducer
Desethylamiodarone hydrochloride is a significant active metabolite of Amiodarone, primarily functioning as an autophagy inducer. It is produced through the action of CYP3A isoenzymes and plays a critical role in cellular processes affecting autophagy. This compound is utilized in research applications focusing on cardiovascular pharmacology and cellular stress responses, due to its influence on potassium channels and potential therapeutic implications in arrhythmias. -
Stable Isotope
Amiodarone-d4 hydrochloride is a deuterium-labeled derivative of the Class III antiarrhythmic agent, Amiodarone hydrochloride, which primarily targets the human ether-a-go-go-related gene (hERG) potassium channel with an IC50 of approximately 45 nM. This compound influences vital cellular processes, promoting fibroblast proliferation and myofibroblast differentiation through the activation of ERK1/2 and p38 MAPK signaling pathways. Amiodarone-d4 hydrochloride is an essential tool for research into supraventricular and ventricular arrhythmias, providing valuable insights into arrhythmia mechanisms and potential therapeutic strategies. -
Stable Isotope
Amiodarone-d10 hydrochloride is a deuterium-labeled derivative of Amiodarone. This compound acts primarily as an antiarrhythmic agent, exerting its effects through the inhibition of ATP-sensitive potassium channels, with an IC50 value of 19.1 μM. It is utilized in pharmacokinetic studies and research focused on cardiovascular diseases, providing insights into drug metabolism and action mechanisms. -
Histamine H1 Receptor/TRPV1 Inhibitor
Dexbrompheniramine is a dual inhibitor of the histamine H1 receptor and the TRPV1 receptor, enabling it to effectively cross the blood-brain barrier. It functions by blocking H1 receptor activity and inhibiting TRPV1-mediated calcium responses in a dose-dependent manner, including responses triggered by Capsaicin. Research indicates that Dexbrompheniramine, when combined with Cimetidine, can mitigate drinking behavior induced by histamine and sham feeding, while it alone does not induce thirst. This compound is valuable for investigating the pathophysiology of chronic cough and related disorders. -
Stable Isotope
Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health. -
Stable Isotope
Rabeprazole-d3 sodium is a deuterium-labeled form of the second-generation proton pump inhibitor, Rabeprazole sodium, which irreversibly inhibits the gastric H+/K+-ATPase. This compound has been shown to induce apoptosis and acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 value of 0.3 μM. Rabeprazole-d3 sodium is utilized in research involving gastric ulcerations and gastroesophageal reflux disorders. -
Stable Isotope
Pantoprazole-d8 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that targets H+/K+-ATPase with an IC50 of 6.8 μM. This compound exhibits significant anti-secretory and anti-ulcer activities, enhancing gastric pH stability. Research applications include investigating the pharmacokinetics of Pantoprazole and its potential synergistic effects with other chemotherapeutic agents, such as Doxorubicin, in tumor growth modulation. -
TRPV1 Antagonist
DWP-05195 is a TRPV1 antagonist that inhibits pain signal transduction, providing research applications in pain management studies. Additionally, DWP-05195 induces endoplasmic reticulum (ER) stress-dependent apoptosis in human ovarian cancer cells, mediated by the ROS-p38-CHOP signaling pathway. This compound may be useful for investigating both nociceptive mechanisms and potential therapeutic strategies for ovarian cancer. -
Stable Isotope
Rabeprazole-13C,d3 is a deuterated form of Rabeprazole, a second-generation proton pump inhibitor (PPI) that irreversibly inhibits gastric H+/K+-ATPase. This compound is known to induce apoptosis and has been identified as an inhibitor of uridine nucleoside ribohydrolase (UNH) with an IC50 value of 0.3 μM. Rabeprazole-13C,d3 is utilized in research focused on gastric ulcerations and gastroesophageal reflux disease, facilitating the study of drug metabolism and action in biological systems. -
Stable Isotope
Pantoprazole-d3 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that selectively targets the H+/K+-ATPase enzyme, exhibiting an IC50 of 6.8 μM. This compound enhances gastric pH stability and demonstrates significant anti-secretory and anti-ulcer properties. It is utilized in research to study gastric acid secretion mechanisms and to investigate potential synergistic effects with chemotherapeutic agents, such as Doxorubicin, in cancer treatment. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
Antiarrhythmic Agent
Quinidine sulfate is an antiarrhythmic agent that primarily targets cardiac ion channels, particularly potassium channels. It exhibits potent K+ channel blocking activity with an IC50 of 19.9 μM and has been shown to induce apoptosis in various cell types. Additionally, quinidine sulfate is utilized in malaria research, making it valuable for studies related to both cardiovascular and infectious diseases. -
Antiarrhythmic Agent
Quinidine polygalacturonate is an antiarrhythmic agent that primarily targets potassium channels, exhibiting an IC50 of 19.9 μM. It also functions as a selective inhibitor of cytochrome P450db and has the capability to induce apoptosis. This compound is particularly useful in research focused on cardiac arrhythmias and malaria studies, making it a valuable reagent for pharmacological investigations. -
Vasodilator
KMUP-1 is a xanthine derivative that acts as a vasodilator through the inhibition of phosphodiesterase (PDE) and activation of soluble guanylyl cyclase (sGC). It stimulates the nitric oxide/sGC/cyclic GMP signaling pathway and facilitates the opening of potassium channels. Additionally, KMUP-1 has been shown to reduce ischemia-induced cardiomyocyte apoptosis. This compound is relevant for studies in cardiovascular health and anti-inflammatory research. -
P-glycoprotein Inhibitor
P-gp inhibitor 22 is a potent inhibitor of P-glycoprotein (P-gp), effectively blocking its efflux function. This compound has been shown to induce apoptosis and promote the accumulation of MCF-7/ADR cells in the S phase of the cell cycle. Its ability to inhibit P-gp makes it relevant in studies focused on multidrug resistance and cancer therapeutics. -
Potassium Channel Inhibitor
DPO-1 is a selective inhibitor of Kv1.5 and Kv1.3 potassium channels (EC50 = 3.1 μM) with notable immunomodulatory and anti-inflammatory properties. It effectively reduces Kv1.3 current density, diminishes Ca2+ influx in calcium-depleted Jurkat cells, and inhibits IL-2 secretion in activated Jurkat cells. Additionally, DPO-1 obstructs uric acid sodium (MSU)-induced NLRP3 inflammasome activation by interfering with Kv1.5-mediated K+ efflux. This reagent is valuable for research into immunological disorders and atrial fibrillation. -
TRPM2 Activator
Adenosine 5′-diphosphoribose sodium is a potent activator of the TRPM2 cation channel, which is permeable to Ca2+. This NAD+ metabolite plays a crucial role in cellular signaling and has been shown to enhance autophagy. It serves as a valuable tool for research investigating calcium signaling pathways and the modulation of autophagy in various biological contexts. -
TRPML1/3 Inhibitor
(rel)-ML-SI3 is a selective inhibitor of TRPML1 and TRPML3, exhibiting IC50 values of 3.1 μM and 28.5 μM, respectively. In contrast, it acts as a potent activator of TRPML2 with an EC50 of 3.3 μM. This compound is valuable for research into the roles of TRPML channels in cellular processes and potential therapeutic interventions in related pathologies. Its specificity for multiple isoforms contributes to its utility in exploring calcium signaling pathways and lysosomal function. -
Antidiabetic Agent
4-Hydroxytolbutamide is a metabolite of Tolbutamide and acts primarily as an antidiabetic agent. It is involved in glucose metabolism by functioning as a potassium channel blocker, influencing insulin secretion from pancreatic beta-cells. This compound is particularly relevant in diabetes research, where it is used to study the pharmacodynamics and pharmacokinetics of sulfonylurea derivatives. Additionally, its metabolism by CYP2C8 and CYP2C9 contributes to understanding drug interactions in antidiabetic therapies. -
L-type Calcium Channel Blocker
Fendiline is an L-type calcium channel blocker that exhibits an IC50 of 17 µM. In addition to its role in cardiovascular modulation, Fendiline acts as a selective inhibitor of K-Ras, with an IC50 of 9.64 μM, effectively preventing K-Ras plasma membrane localization and blocking downstream signaling. This compound has demonstrated potential in inhibiting the proliferation of various cancer cell lines such as pancreatic, colon, lung, and endometrial cancers that express oncogenic mutant K-Ras. Furthermore, Fendiline serves as a STING agonist, showing promise in inhibiting the growth of refractory cold tumors, including MC38, CT26, and B16F10. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine dihydrochloride is a potent antimicrobial agent that acts primarily by intercalating into bacterial DNA, disrupting replication and transcription, and leading to bacterial cell lysis. Additionally, it serves as a Kir3.2 potassium channel blocker, making it a valuable tool for investigating neurological conditions such as Down syndrome. Furthermore, due to its ability to penetrate skin layers and accumulate in the cell nucleus, long-term exposure requires careful handling due to potential carcinogenic effects. This reagent is applicable in studies concerning microbial resistance and neurological phenotype exploration. -
Anti-microbial Agent/Kir3.2 Blocker
3,6-Diaminoacridine sulfate functions primarily as an anti-microbial agent and a Kir3.2 potassium channel blocker. This acridine compound exhibits broad-spectrum antibacterial activity by intercalating into bacterial DNA, disrupting replication and transcription, ultimately leading to cell lysis. Additionally, it is utilized in neurological research, particularly in studying the phenotype associated with Down syndrome. Notably, 3,6-Diaminoacridine sulfate exhibits the capability to penetrate the skin's stratum corneum and accumulate in the cell nucleus, with prolonged exposure possibly linked to carcinogenic effects. -
Sodium Channel Inhibitor
Articaine is a selective inhibitor of voltage-gated sodium channels, including rNav1.4, hNav1.7, and rNav1.8, demonstrating an IC50 of 15.8 μM for open-state Na+ channels. It effectively blocks Na+ influx, leading to local anesthetic effects and interruption of nerve impulse conduction. Additionally, Articaine exhibits anti-inflammatory properties by inhibiting NF-κB activation and the NLRP3 inflammasome pathway. This compound is valuable for research in dental anesthesia and inflammatory-related conditions, such as acute kidney injury. -
CO Donor
Tricarbonyldichlororuthenium(II) dimer serves as a carbon monoxide (CO) donor, facilitating various biological processes. This compound demonstrates notable anti-inflammatory and antioxidant properties, in addition to its protective effects on gastric mucosa. Furthermore, Tricarbonyldichlororuthenium(II) dimer exhibits CO-independent effects on several potassium channels, highlighting its significance in cellular physiology and potential therapeutic applications. -
NAAA Inhibitor
AM9053 is a selective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) with an IC50 of 30 nM. It shows limited impact on FAAH activity (IC50 > 100 nM). AM9053 demonstrates significant anti-proliferative effects on colorectal cancer cells through the activation of PPAR-α and TRPV1-dependent pathways, leading to S-phase cell cycle arrest. Additionally, it alleviates intestinal fibrosis by modulating macrophage activity and inhibiting the IL-23 signaling pathway, resulting in increased levels of N-acylethanolamines, particularly palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). AM9053 is valuable for research into colorectal cancer and intestinal fibrosis. -
ABCG2/BCRP Inhibitor
Triclabendazole sulfoxide is an ABCG2/BCRP inhibitor that serves as the primary plasma metabolite of Triclabendazole. This compound demonstrates significant anti-parasitic activity and is useful in research applications focusing on the modulation of drug transport mechanisms in cellular assays. It contributes to studies investigating the role of ABCG2/BCRP in drug resistance and pharmacokinetics. -
Mycotoxin
Roquefortine C is a mycotoxin derived from Penicillium species, exhibiting multiple biological activities. As an agonist of P-glycoprotein (P-gp), it inhibits cytochrome P450 enzymes, specifically P450 3A and P450 1A. This compound demonstrates antimicrobial effects against Gram-positive bacteria and possesses neurotoxic properties, along with potential antitumor activity. Roquefortine C serves as a valuable tool in research exploring microbial interactions and pharmacological mechanisms. -
HSP70 ATPase Inhibitor
Displurigen (NSC375009) is an HSP70 ATPase inhibitor that specifically targets HSPA8, disrupting the pluripotency of human embryonic stem cells. This compound effectively inhibits the ATPase activity of HSP70 with an IC50 of 225 μM, making it a valuable tool for research in stem cell biology and differentiation processes. Its mechanism of action provides insights into cellular signaling pathways related to stem cell maintenance and development. -
ASH ATPase Activity Inhibitor
SEW84 is a potent inhibitor of Aha1-stimulated Hsp90 (ASH) ATPase activity, demonstrating an IC50 of 0.3 μM. This compound is valuable for investigating the role of Hsp90 in protein deposition disorders and offers insights into the underlying mechanisms of these diseases. Additionally, SEW84 may serve as a tool for studying Hsp90's involvement in cellular stress responses and protein folding pathways. -
CFTR
H2-Gamendazole, a derivative of Lonidamine, targets the cystic fibrosis transmembrane conductance regulator (CFTR). It demonstrates significant efficacy in reducing cyst formation in polycystic kidney disease models. This compound is primarily used in research related to autosomal dominant polycystic kidney disease, contributing to a better understanding of therapeutic strategies for this condition. -
Endogenous Metabolite
UCCF-029 free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. This compound showcases enhanced activity due to the benzannulation of the flavone A-ring at the 7,8-position, serving as a critical structural reference for the development of more effective flavonoid analogues. UCCF-029 demonstrates superior potency compared to apigenin in activating wild-type CFTR and possesses potential for activating the mutant G551D-CFTR, though its efficacy in this regard is not as pronounced as that of apigenin. This reagent is valuable for research into cystic fibrosis and related therapeutic strategies. -
Endogenous Metabolite
ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions. -
Endogenous Metabolite
D-myo-Inositol-1,4,5,6-tetraphosphate (D-Ins(1,4,5,6)P4) functions primarily as an endogenous metabolite involved in cellular signaling pathways. This compound exhibits a strong inhibitory effect on calcium-activated chloride channels, effectively operating at concentrations of 8-10 μM. It is commonly utilized in research applications focused on signal transduction and ion channel regulation. -
Biochemical Reagent
D-myo-Inositol-4,5-diphosphate sodium is a critical biochemical reagent that functions as a second messenger in cellular signaling pathways. It primarily targets calcium channels, facilitating the release of intracellular calcium when it binds to its receptor on the endoplasmic reticulum. This compound is valuable for research applications investigating signal transduction, calcium homeostasis, and cellular responses in various biological systems. -
Endogenous Metabolite
Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications. -
Endogenous Metabolite
SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways. -
Furin Inhibitor
BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions. -
Sodium Channels Blocker
Phrixotoxin 3 is a selective blocker of voltage-gated sodium channels, demonstrating IC50 values of 0.6 nM for NaV1.2, 42 nM for NaV1.3, 72 nM for NaV1.4, 288 nM for NaV1.1, and 610 nM for NaV1.5. This compound modulates sodium channel activity by shifting gating kinetics in a depolarized direction while inhibiting the inward sodium current. Phrixotoxin 3 is valuable for research focusing on ion channel modulation, neurophysiology, and the investigation of sodium channel-related pathologies. -
Sodium Current Blocker
F-15845 hydrobromide is a potent persistent sodium current blocker, primarily targeting voltage-gated sodium channels. It demonstrates significant cardioprotective properties and anti-ischemic activity, providing both short- and long-term protection following myocardial infarction. This compound is valuable for investigating functional impairments in the myocardium and exploring therapeutic strategies related to cardiac health. -
Sodium Channel Antagonist
Hainantoxin-IV is an antagonist of voltage-gated sodium channels, specifically targeting tetrodotoxin-sensitive (TTX-S) subtypes. This compound exhibits potent inhibitory activity through its interaction with key residues His28 and Lys32, which facilitate binding to the sodium channel. Hainantoxin-IV, characterized by an inhibitor cystine knot motif, is valuable in research applications exploring sodium channel modulation and related neurophysiological processes. -
AMPAR Agonist
(S)-(-)-5-Fluorowillardiine hydrochloride is a selective agonist of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR). This compound exhibits significant biological activity by enhancing synaptic transmission and promoting excitatory neurotransmission in the central nervous system. It is valuable for research applications focused on studying synaptic plasticity, neurophysiology, and potential therapeutic interventions in neurological disorders related to glutamate signaling. -
AMPA Receptor Modulator
AMPA Receptor Modulator-8 selectively modulates AMPA receptors, exhibiting an IC50 of 0.02 nM for TARP-γ2. This compound plays a significant role in the investigation of neurological disorders such as epilepsy, Alzheimer's disease, and Parkinson's disease. Its precise action on AMPA receptor dynamics makes it a valuable tool for advancing research in neuropharmacology and therapeutic development. -
AMPA-type Receptors Positive Allosteric Modulator
S 18986 is a selective positive allosteric modulator of AMPA-type receptors, demonstrating significant brain penetration and oral bioavailability. This compound enhances cognitive function in rodent models, evidenced by its ability to activate the release of noradrenaline and acetylcholine in the rat hippocampus. S 18986 has shown efficacy in improving memory performance in object-recognition tests, making it a valuable tool for research into cognitive enhancement and neuropharmacology. -
AMPA Receptor Antagonist
Selurampanel is a competitive antagonist of the AMPA receptor, demonstrating an IC50 of 190 nM. This compound exhibits significant penetration of the blood-brain barrier, making it suitable for in vivo studies. Selurampanel is primarily employed in research related to epilepsy, providing insights into neuroprotective mechanisms and potential therapeutic applications.
