Isotope-Labeled Compounds

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  1. Stable Isotope

    Ropivacaine-d7 is a deuterium-labeled derivative of Ropivacaine, a potent sodium channel blocker. It works by reversibly inhibiting sodium ion influx, thereby blocking impulse conduction in nerve fibers. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is primarily used in studies focused on the management of neuropathic pain.
  2. Stable Isotope

    Minoxidil-d10 is a deuterium-labeled analogue of Minoxidil, primarily functioning as an ATP-sensitive potassium (KATP) channel opener. This compound exhibits potent antihypertensive properties and functions as a peripheral vasodilator, enhancing vasodilation and influencing hair growth. Additionally, Minoxidil-d10 serves as a significant inhibitor of soybean lipoxygenase, with an IC50 of 20 μM, making it valuable for research applications in cardiovascular science and dermatology.
  3. Stable Isotope

    Nicorandil-d4 is the deuterium-labeled analog of Nicorandil, a potent activator of potassium channels, specifically targeting vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). This compound exhibits significant vasodilatory and cardioprotective effects, making it relevant for research in angina and ischemic heart diseases. Nicorandil-d4 serves as a valuable stable isotope for metabolism studies and pharmacokinetic investigations in cardiovascular research.
  4. Stable Isotope

    Glipizide-d11 is a deuterium-labeled derivative of Glipizide, a sulfonylurea-class anti-diabetic agent. It demonstrates potent activity in the management of type 2 diabetes mellitus by partially inhibiting ATP-sensitive potassium (KATP) channels in the β cells of the pancreatic islets of Langerhans. This stable isotope form is utilized in pharmacokinetic studies and metabolic research, helping to better elucidate the drug's pharmacodynamics and biological interactions.
  5. Stable Isotope

    Gliclazide-d4 is a deuterated analog of Gliclazide, a recognized inhibitor of ATP-sensitive potassium channels in pancreatic beta cells. It exhibits biological activity as an antidiabetic agent with an IC50 of 184 nM, effectively regulating insulin secretion. Gliclazide-d4 is suitable for pharmacokinetic studies, metabolic research, and tracer studies in glucose homeostasis investigations.
  6. Stable Isotope

    Vernakalant-d6 hydrochloride is a deuterium-labeled analogue of Vernakalant, primarily used as a stable isotope in research applications. This compound facilitates investigations into the pharmacokinetics and metabolic pathways of Vernakalant by enabling the tracking of molecular interactions and dynamics in biological systems. Researchers can utilize Vernakalant-d6 hydrochloride in studies related to cardiac arrhythmias and antiarrhythmic drug mechanisms.
  7. Stable Isotope

    (Rac)-Ropivacaine-d7 is a deuterium-labeled analogue of (Rac)-Ropivacaine, a local anesthetic that primarily acts by blocking voltage-gated sodium channels. This stable isotope is valuable in pharmacokinetic studies and metabolic research, enabling researchers to investigate the drug's distribution, metabolism, and elimination in biological systems. The incorporation of deuterium enhances the sensitivity and specificity of analytical methods such as mass spectrometry.
  8. Stable Isotope

    Amifampridine-d3 (3,4-Diaminopyridine-d3) is a deuterium-labeled analog of Amifampridine, a potent and cell-permeable blocker of voltage-gated potassium (Kv) channels. This compound enhances neurotransmitter release at neuromuscular junctions, making it effective in the reversal of botulinum toxin A (BoNT/A) intoxication. Amifampridine-d3 is also valuable for research into Lambert-Eaton myasthenic syndrome (LEMS), providing insights into neuromuscular transmission and associated pathophysiology.
  9. Stable Isotope

    Dehydroindapamide-d3 is a deuterium-labeled derivative of Dehydroindapamide, targeting cytochrome P450 enzyme CYP3A4. This stable isotope standard is designed for the quantitative assessment of Indapamide turnover rates, demonstrating a turnover rate roughly 10-fold greater than Indoline and showing enhanced affinity for CYP3A4. It is a valuable tool in pharmacokinetic studies and can aid in drug metabolism research.
  10. Stable Isotope

    Acetohexamide-d11 is a deuterium-labeled derivative of Acetohexamide, a first-generation sulfonylurea compound. This reagent primarily targets ATP-sensitive potassium channels in pancreatic β cells, promoting insulin secretion vital for studies on type 2 diabetes. Researchers can utilize Acetohexamide-d11 to trace metabolic pathways and evaluate pharmacokinetics in diabetes research applications.
  11. Stable Isotope

    Mesoridazine-d3 is a deuterium-labeled derivative of Mesoridazine, a phenothiazine antipsychotic that primarily targets human ether-a-go-go related gene (hERG) channels. This compound functions as a rapid open-channel blocker of hERG currents, exhibiting an IC50 value of 550 nM in human embryonic kidney 293 cells. Mesoridazine-d3 is useful in pharmacological studies related to schizophrenia and other psychiatric disorders, facilitating research into the mechanisms underlying these conditions.
  12. Stable Isotope

    Ropivacaine-d7 hydrochloride is a deuterium-labeled derivative of Ropivacaine, primarily functioning as a potent sodium channel blocker. It inhibits sodium ion influx in nerve fibers, leading to reversible blockade of impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the TREK-1 potassium channel, demonstrating an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is valuable for research in neuropathic pain management and the study of ion channel dynamics.
  13. Stable Isotope

    L-Palmitoylcarnitine-d3-1 hydrochloride is a deuterated form of L-Palmitoylcarnitine, a long-chain acylcarnitine known for its role in fatty acid metabolism. This reagent contributes to the understanding of membrane lipid dynamics during ischaemic conditions, where it accumulates in the sarcolemma and disrupts lipid environments. Additionally, L-Palmitoylcarnitine-d3-1 hydrochloride inhibits KATP channel activity through interaction with the Kir6.2 subunit, making it a valuable tool for investigating metabolic pathways and channel function in various research applications.
  14. Stable Isotope

    Indapamide-13C,d3 is a stable isotope-labeled form of the sulphonamide diuretic, Indapamide. This compound primarily acts by lowering blood pressure through the reduction of vascular reactivity and peripheral vascular resistance. Additionally, Indapamide is known to decrease left ventricular hypertrophy, making it useful for cardiovascular research applications, including studies on hypertension and cardiac remodeling.
  15. Stable Isotope

    (rac)-Indapamide-d3 is a stable isotope-labeled derivative of the racemic compound Indapamide. As a sulphonamide diuretic, Indapamide functions primarily by reducing vascular reactivity and peripheral vascular resistance, leading to decreased blood pressure. Additionally, it has been shown to mitigate left ventricular hypertrophy. This isotope-labeled reagent is suitable for pharmacokinetic studies, metabolic analysis, and tracing applications in biological research.
  16. Stable Isotope

    L-Palmitoylcarnitine-d9 is a deuterium-labeled derivative of L-Palmitoylcarnitine, functioning as a stable isotope for biological studies. L-Palmitoylcarnitine plays a critical role in fatty acid metabolism and is known to accumulate in the sarcolemma, where it influences the lipid environment during ischemic conditions. This compound inhibits KATP channel activity by interacting with the Kir6.2 subunit, while not altering single-channel conductance. Its unique properties make it suitable for research in metabolic diseases and cardiac physiology.
  17. Stable Isotope

    Flecainide-d3 is a deuterium-labeled form of Flecainide, a clinically utilized antiarrhythmic agent. Its primary mechanism involves blocking sodium channels while also inhibiting calcium ion release through the cardiac ryanodine receptor (RyR2). This reagent is valuable in research focused on cardiac arrhythmias, particularly in the study of catecholaminergic polymorphic ventricular tachycardia (CPVT) and related cardiac conditions. Its stable isotope labeling facilitates advanced pharmacokinetic and metabolic studies.
  18. Stable Isotope

    Abscisic acid-d6 is a deuterium-labeled derivative of abscisic acid, functioning as a stable isotope. This compound is known for its ability to inhibit the proton pump (H+-ATPase), making it a valuable tool for investigating physiological processes regulated by abscisic acid. Its applications extend to studying plant stress responses, signal transduction pathways, and metabolic regulation in various biological systems.
  19. Stable Isotope

    Esomeprazole-d6 sodium is a deuterium-labeled derivative of Esomeprazole. This compound functions primarily as a proton pump inhibitor, effectively reducing gastric acid secretion by inhibiting the H+, K+-ATPase enzyme in gastric parietal cells. Esomeprazole-d6 sodium is valuable for research applications focused on gastroesophageal reflux disease, enabling the study of metabolic pathways and pharmacokinetics in related therapeutic investigations.
  20. Stable Isotope

    Pantoprazole sulfide-d8 is a deuterated form of Pantoprazole sulfide, acting as a stable isotope analogue. This compound serves as a metabolite of Pantoprazole, a well-known proton-pump inhibitor. Pantoprazole sulfide-d8 is primarily utilized in pharmacokinetic studies to investigate the metabolic pathways and mechanisms of action of proton-pump inhibitors in various biological systems.
  21. Stable Isotope

    Lansoprazole sulfone-d4 is a deuterium-labeled derivative of Lansoprazole sulfone, which functions as a selective inhibitor of H+, K+-ATPase. This compound is significant in the study of various gastrointestinal disorders, including duodenal ulcer, gastric ulcer, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. As a stable isotope, Lansoprazole sulfone-d4 is valuable for metabolic studies and tracing applications in pharmacokinetic research.
  22. Stable Isotope

    Lansoprazole sulfone-13C6 is a stable isotope-labeled form of Lansoprazole sulfone, a known inhibitor of the H+, K+-ATPase enzyme. This compound serves as a valuable metabolic marker for studying the pharmacokinetics and biological effects of Lansoprazole in various conditions, including duodenal and gastric ulcers, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. Its stable isotope labeling allows for precise tracking in metabolic studies and applications in drug formulation research.
  23. Stable Isotope

    Empagliflozin-d4 is a deuterium-labeled derivative of Empagliflozin, a selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor. With an IC50 of 3.1 nM for human SGLT-2, this stable isotope is utilized primarily in pharmacokinetic studies and metabolic research. Its labeling facilitates the investigation of drug metabolism and the tracking of pharmacological effects in biological systems.
  24. Stable Isotope

    Dapagliflozin-d5 is a deuterated form of Dapagliflozin, a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This stable isotope is utilized in metabolic studies and pharmacokinetic research to trace the absorption and distribution of Dapagliflozin in biological systems. Its application in advanced research provides insights into the drug's mechanism and efficacy in managing diabetes.
  25. Stable Isotope

    Canagliflozin-d4 is a deuterium-labeled derivative of Canagliflozin, a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research to trace and quantify the pharmacological fate of Canagliflozin in biological systems. The presence of deuterium allows for enhanced detection and analysis, facilitating investigations into glucose homeostasis and associated therapeutic applications in diabetes management.
  26. Stable Isotope

    Empagliflozin-d8 is a deuterium-labeled derivative of Empagliflozin, a selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor. With an IC50 of 3.1 nM for human SGLT-2, this compound exhibits significant biological activity in glucose regulation and is utilized in diabetes research. Its stable isotope labeling enables enhanced analytical sensitivity and specificity in pharmacokinetic studies and metabolic profiling.
  27. Stable Isotope

    Pragliflozin-13C6 is a stable isotope-labeled form of Ipragliflozin, a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor. This compound demonstrates inhibitory activity with IC50 values of 7.38 nM for human SGLT2 and significantly higher values for SGLT1, making it a potent antidiabetic agent. Pragliflozin-13C6 is primarily utilized in pharmacokinetic studies and metabolic experiments to trace the pathways and mechanisms of Ipragliflozin in biological systems.
  28. Stable Isotope

    Ertugliflozin-d5 is a deuterium-labeled form of Ertugliflozin, a selective and potent inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2). With an IC50 of 0.877 nM against human SGLT2, it effectively reduces glucose reabsorption in the kidneys, making it relevant in research aimed at understanding type 2 diabetes mellitus treatment mechanisms. This stable isotope-labeled reagent is valuable for pharmacokinetic studies and metabolic tracing in biological systems.
  29. Stable Isotope

    Remogliflozin etabonate-d7 is the deuterium-labeled variant of Remogliflozin etabonate, a selective sodium glucose cotransporter 2 (SGLT2) inhibitor. With Ki values of 1.95 μM for hSGLT2 and 2.14 μM for rSGLT2, it demonstrates notable inhibition of glucose reabsorption in renal tissues. Remogliflozin etabonate is metabolized to its active form within the body, contributing to its antidiabetic effects observed in rodent models. This stable isotope-labeled compound is valuable for pharmacokinetic studies and metabolic research involving SGLT2 inhibition.
  30. Stable Isotope

    Dapagliflozin-d4 is a stable isotope-labeled form of Dapagliflozin, an SGLT2 inhibitor that effectively targets sodium/glucose cotransport in the treatment of diabetes mellitus (DM). This compound promotes glucose excretion via urine, contributing to improved glycemic control. Additionally, Dapagliflozin has been shown to induce HIF1 expression and mitigate renal ischemia-reperfusion injury, making it a valuable tool for research in diabetic complications and renal protection mechanisms.
  31. Stable Isotope

    Triamterene-d5 is a deuterium-labeled derivative of Triamterene, functioning primarily as a stable isotope for analytical purposes. It acts as a blocker of the epithelial Na+ channel (ENaC) in a voltage-dependent manner, serving as a mild diuretic. Additionally, Triamterene demonstrates inhibitory activity at the TGR5 receptor, making it valuable for research into renal function and metabolic processes.
  32. Stable Isotope

    Benzocaine-(ethyl-d5) is a deuterated form of benzocaine, targeting voltage-gated Na+ channels. This stable isotope serves as a valuable tool in pharmacokinetic studies and mechanistic research, enabling precise tracking of benzocaine metabolism and dynamics in biological systems. Its inhibitory concentration (IC50) is reported at 0.8 mM when assessed at a membrane potential of +30 mV, making it relevant for investigations into local anesthetic mechanisms and interactions.
  33. Stable Isotope

    Alvimopan-d7 is a deuterium-labeled variant of Alvimopan, a potent and selective oral μ-opioid receptor antagonist. With an IC50 of 1.7 nM, Alvimopan exhibits significant selectivity for the μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors, with Kis of 100 nM and 12 nM, respectively. This stable isotope-labeled compound is valuable for research applications focused on postoperative ileus and opioid receptor pharmacology.
  34. Isotope-Labeled Compound

    O,O-Diethyl dithiophosphate-13C4 ammonium is a stable isotope-labeled compound used primarily in chemical and biological research. It serves as a useful tool for tracing and quantifying metabolic pathways in various biological systems due to its incorporation of the carbon-13 isotope. This compound aids in the study of organophosphate interactions and can enhance the understanding of biochemical mechanisms and environmental fate of similar thiophosphate agents.
  35. Stable Isotope

    O-Desmethyltramadol-d6 hydrochloride is a deuterated stable isotope of O-Desmethyltramadol hydrochloride, the principal active metabolite of tramadol. This compound is capable of traversing the blood-brain barrier and primarily exerts its analgesic effects through activation of the µ-opioid receptor (µ-OR). O-Desmethyltramadol-d6 hydrochloride is valuable in pharmacokinetic studies and tracer research due to its isotopic labeling, offering precise tracking in biological systems.
  36. Stable Isotope

    Ticagrelor-d7 is a deuterium-labeled derivative of Ticagrelor, a reversible P2Y12 receptor antagonist. This stable isotope is utilized in research for studying platelet aggregation and related cardiovascular processes. Its unique labeling enables precise tracking and quantification in various biochemical assays, enhancing the understanding of antiplatelet therapies in clinical and experimental settings.
  37. Stable Isotope

    Prasugrel-d3 is a deuterium-labeled form of Prasugrel, a thienopyridine prodrug that selectively antagonizes the P2Y12 receptor. This compound effectively inhibits ADP-induced platelet aggregation, thereby demonstrating significant platelet-inhibitory activity. Prasugrel-d3 is valuable for studying platelet function and the pharmacokinetics of Prasugrel in various biological research applications.
  38. Stable Isotope

    Uridine 5′-diphosphoglucose-13C6 disodium is a stable isotope-labeled form of Uridine 5′-diphosphoglucose. It functions primarily as a potent agonist of the proinflammatory P2Y14 receptor, playing a crucial role in modulating inflammation and neutrophil polarization. This compound is significant for research applications in understanding cellular responses to ischemia and reperfusion, particularly in myocardial infarction models. Additionally, it serves as a precursor for glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids, making it valuable for various biochemical studies.
  39. Stable Isotope

    Prasugrel-13C6 is a stable isotope-labeled form of Prasugrel, a thienopyridine compound classified as a prodrug. It functions as a potent P2Y12 receptor antagonist, effectively inhibiting ADP-induced platelet aggregation, thereby reducing platelet activation and aggregation in cardiovascular settings. This reagent is valuable for research applications involving pharmacokinetics, metabolism studies, and mechanisms of platelet inhibition.
  40. Stable Isotope

    Clopidogrel-13C,d3 sulfate is a stable isotope-labeled version of (±)-Clopidogrel bisulfate, primarily functioning as a platelet P2Y12 receptor inhibitor and ADP receptor antagonist. It inhibits the binding of adenosine diphosphate (ADP) to its receptors on platelet membranes, thereby blocking ADP-mediated activation of the GPIIb/IIIa complex. This compound demonstrates significant potential in reducing vascular inflammation and attenuating progression of angiotensin II-induced abdominal aortic aneurysms, in addition to exhibiting anti-inflammatory properties. It is utilized in various research applications focused on platelet aggregation and cardiovascular health.
  41. Stable Isotope

    (±)-Clopidogrel-d4 is a deuterium-labeled derivative of (±)-Clopidogrel, a selective platelet P2Y12 receptor inhibitor and adenosine diphosphate (ADP) receptor antagonist. This compound effectively prevents ADP binding to platelet receptors, thereby inhibiting ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel-d4 is utilized in research related to vascular inflammation and the progression of conditions such as angiotensin II-induced abdominal aortic aneurysms, and it also exhibits notable anti-inflammatory properties.
  42. Stable Isotope

    Prasugrel-d4 is a deuterated analog of Prasugrel, a thienopyridine compound that acts as a potent P2Y12 receptor antagonist. By inhibiting ADP-induced platelet aggregation, Prasugrel is utilized in various research applications related to cardiovascular diseases and thrombosis studies. The stable isotope labeling allows for advanced pharmacokinetic and metabolic investigations, facilitating deeper insights into the drug's mechanism of action and its effects on platelet function.
  43. Stable Isotope

    Prasugrel-d5 is a deuterium-labeled variant of Prasugrel, a thienopyridine prodrug that functions as a potent inhibitor of platelet aggregation. By acting as an antagonist of the P2Y12 receptor, Prasugrel-d5 effectively inhibits ADP-induced platelet activation. This stable isotope can be used in pharmacokinetic studies and metabolic profiling to enhance understanding of drug metabolism and therapeutic effects in cardiovascular research.
  44. Stable Isotope

    Clopidogrel-d3 hydrogen sulfate is a deuterated form of Clopidogrel hydrogen sulfate, primarily designed as a stable isotope for pharmacokinetic studies. This compound functions as a potent antiplatelet agent, preventing blood clot formation by inhibiting platelet aggregation induced by ADP. Clopidogrel-d3 hydrogen sulfate also selectively inhibits cytochrome P450 isoforms CYP2B6 and CYP2C19, with IC50 values of 18.2 nM and 524 nM, respectively. Its usage is instrumental in research involving antithrombotic therapies and drug metabolism.
  45. Stable Isotope

    Uridine 5′-diphosphoglucose-13C disodium is a stable isotope-labeled form of Uridine 5′-diphosphoglucose (UDP-glucose). This compound functions as a potent agonist for the proinflammatory P2Y14 receptor, playing a critical role in modulating inflammation and the polarization of neutrophils. Additionally, UDP-glucose is a key precursor for the synthesis of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in both animal tissues and select microorganisms. It holds potential for research applications focused on mitigating inflammation associated with myocardial infarction and reperfusion injury in cardiac tissue.
  46. Stable Isotope

    Ticagrelor-d4 is a deuterium-labeled derivative of Ticagrelor, functioning as a reversible oral P2Y12 receptor antagonist. This stable isotope is primarily utilized in pharmacokinetic and metabolic studies, providing a valuable tool for investigating pharmacodynamics and the pharmacological effects of Ticagrelor. Its application in research facilitates a deeper understanding of platelet aggregation mechanisms and the drug's therapeutic efficacy.
  47. Stable Isotope

    (±)-Clopidogrel-d7 sulfate is a stable isotope-labeled derivative of (±)-Clopidogrel sulfate, featuring deuterium substitution. This compound serves as an important tool in pharmacokinetic studies and drug metabolism research, facilitating the investigation of clopidogrel's biotransformation and biological activity. Its isotopic labeling enables detailed analysis in mass spectrometry applications, providing insights into drug interactions and therapeutic efficacy.
  48. Stable Isotope

    Rac-Fesoterodine-d14 fumarate is a stable isotope-labeled version of the racemic muscarinic receptor antagonist Fesoterodine. It exhibits competitive inhibition across multiple mAChR subtypes, with pKivalues of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This compound is primarily utilized in research applications focusing on the pharmacological characterization and monitoring of overactive bladder treatments.
  49. Stable Isotope

    (R)-Oxybutynin-d10 is a deuterium-labeled derivative of (R)-Oxybutynin, a racemic isomer known for its role as a muscarinic receptor antagonist. This compound exhibits antispasmodic, antimuscarinic, and anticholinergic properties, effectively competing with carbachol-induced contractions. (R)-Oxybutynin-d10 is utilized in research related to urinary incontinence and neurogenic bladder dysfunction, facilitating the study of mechanisms underlying these conditions.
  50. Stable Isotope

    Biperiden-d5 is a deuterium-labeled analog of Biperiden, a non-selective muscarinic receptor antagonist that primarily targets M1 muscarinic receptors. By competitively binding to these receptors, Biperiden-d5 inhibits acetylcholine signaling, which can enhance dopaminergic activity within the central nervous system. This stable isotope is valuable for research applications related to Parkinson's disease and associated neuropsychiatric disorders, providing insights into receptor interactions and signaling pathways.

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