Isotope-Labeled Compounds

L-Palmitoylcarnitine-d3 hydrochloride is the deuterium-labeled form of L-Palmitoylcarnitine hydrochloride, which serves as a stable isotope in research applications. This long-chain acylcarnitine plays a crucial role in fatty acid metabolism and is known to accumulate in the sarcolemma, disrupting membrane lipid composition during ischemic conditions. Additionally, L-Palmitoylcarnitine hydrochloride inhibits KATP channel activity via interaction with the Kir6.2 subunit, providing valuable insights for studies on cardiac health and metabolic disorders.

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.

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.

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.

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.

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.

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.

(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.

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.

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.

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.

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.

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.

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.

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.

(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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

Decanoic acid-d3 is a deuterium-labeled derivative of decanoic acid, which serves as a stable isotope for research applications. As a component of medium-chain triglycerides, it is known for its ability to penetrate the blood-brain barrier and act as a non-competitive inhibitor of AMPA receptors. Its biological activity includes antiseizure effects, making it a valuable tool for studies related to neuropharmacology and epilepsy research.

Glycine-2-13C,15N is a stable isotope-labeled form of glycine that incorporates both 13C and 15N isotopes. Glycine serves as an inhibitory neurotransmitter in the central nervous system and functions as a co-agonist with glutamate, enhancing excitatory signaling at NMDA receptors. This reagent is valuable for metabolic studies, tracing pathways of glycine metabolism, and investigating neurotransmitter dynamics in neurological research.

Glycine-d3 is a deuterium-labeled form of glycine, an important inhibitory neurotransmitter in the central nervous system (CNS). It serves as a co-agonist with glutamate, enhancing excitatory signaling at NMDA receptors. Glycine-d3 is valuable for studying neurotransmission, metabolic pathways, and isotopic labeling in various biochemical and pharmacological research applications.

Felbamate-d4 is a deuterated analog of Felbamate, functioning primarily as a stable isotope. It exhibits significant anticonvulsant activity, which is thought to result from its inhibition of N-methyl-D-aspartate (NMDA) receptors. This reagent is valuable in pharmacokinetic studies and metabolic labeling applications, facilitating detailed investigations into the drug's mechanisms and effects in neurological research.

Quinolinic acid-13C3,15N is a stable isotope-labeled derivative of quinolinic acid, classified as 2,3-Pyridinedicarboxylic Acid-13C3,15N. This compound acts as an agonist for N-methyl-D-aspartate (NMDA) receptors and is produced through the metabolism of L-tryptophan via the kynurenine pathway. Quinolinic acid-13C3,15N is valuable for research investigating NMDA receptor-mediated neuronal damage and dysfunction, enabling the study of neurobiology and related disorders.

Glycine-1-13C,15N is a stable isotope-labeled form of glycine, featuring carbon-13 and nitrogen-15 isotopes. Glycine functions as an inhibitory neurotransmitter in the central nervous system (CNS) and serves as a co-agonist with glutamate at the N-methyl-D-aspartic acid (NMDA) receptors, enhancing excitatory synaptic transmission. This labeled compound is essential for research in metabolic studies, neuropharmacology, and the evaluation of neurotransmitter dynamics in various biological processes.

Glycine-15N,d2 is a stable isotope-labeled form of glycine, incorporating deuterium and nitrogen-15 isotopes. Glycine functions as an inhibitory neurotransmitter in the central nervous system and serves as a co-agonist with glutamate at NMDA receptors, promoting excitatory signaling. This isotopically enriched reagent is valuable for studies involving metabolic pathways, molecular labeling, and neurochemical research applications.

CX516-d10 is a deuterated form of CX516, functioning as an ampakine and a positive allosteric modulator of AMPA receptors. This compound is significant for research into neurological disorders such as Alzheimer's disease, schizophrenia, and mild cognitive impairment (MCI), providing valuable insights into the modulation of cognitive functions and synaptic transmission. Its stable isotope labeling facilitates advanced studies in pharmacokinetics and metabolic profiling.

Glycine-13C2,15N,d2 is a stable isotope-labeled form of Glycine, incorporating deuterium, carbon-13, and nitrogen-15. Glycine functions as an inhibitory neurotransmitter in the central nervous system while also acting as a co-agonist with glutamate at the NMDA receptors, enhancing excitatory signaling. This labeled compound is valuable for metabolic studies, tracer experiments, and isotopic labeling in various biochemical and neurobiological research applications.

N,N-Dimethylglycine-d3 hydrochloride is a deuterium-labeled derivative of N,N-Dimethylglycine hydrochloride, primarily utilized as a stable isotope in research. This compound functions as a partial agonist at the N-methyl-D-aspartate receptor (NMDAR) glycine binding site, making it valuable for studies related to neurotransmission and receptor signaling. Additionally, N,N-Dimethylglycine-d3 has been shown to possess immunomodulatory properties and may aid in antioxidant defense by mitigating oxidative stress. Its applications extend to research in mental health and surfactant activity.

Indole-2-carboxylic acid-13C is a stable isotope-labeled variant of Indole-2-carboxylic acid, which acts as a potent inhibitor of lipid peroxidation. It specifically and competitively inhibits the glycine-mediated potentiation of NMDA receptor-gated currents, making it a valuable tool for investigating excitatory neurotransmission and oxidative stress pathways. This compound is suitable for applications in pharmacological research and metabolic studies focusing on neuroprotection and lipid metabolism.

Memantine-d3 hydrochloride is a deuterium-labeled analog of Memantine, a noncompetitive antagonist of the N-methyl-D-aspartate receptor (NMDAR). This stable isotope is utilized in research on moderate-to-severe Alzheimer's disease (AD), providing insights into the pharmacokinetics and action of Memantine in a biological context. Memantine's mechanism of action allows for the exploration of glutamatergic signaling pathways relevant to neurodegenerative diseases.

Decanoic acid-d2 is a deuterium-labeled derivative of decanoic acid, a medium-chain triglyceride. It acts as a non-competitive inhibitor of the AMPA receptor, demonstrating notable antiseizure properties. This stable isotope is essential for research applications involving metabolic studies and neuropharmacology, particularly in understanding the mechanisms behind its anticonvulsant effects.

Perfluoroenanthic acid-13C4 is a stable isotope labeled variant of Perfluoroenanthic acid, a perfluoroalkyl substance (PFAS) known for its significant biological implications. This compound has been shown to adversely affect the development of seminiferous tubules and influence m6A RNA methylation in the testes of offspring mice following maternal exposure, which disrupts spermatogenesis and contributes to reproductive toxicity. Additionally, Perfluoroenanthic acid alters dendritic spine morphology and synaptic formation in primary cortical neuron cultures, enhancing neuronal activity, synaptic transmission, and elevating the expression of key excitatory synapse-related proteins, such as Synaptophysin and PSD95, making it valuable for research in neurobiology and developmental toxicology.

Felbamate-d5 is a deuterated analog of Felbamate, a potent nonsedative anticonvulsant primarily targeting the N-methyl-D-aspartate (NMDA) receptor. Its stable isotope labeling allows for enhanced tracking and quantification in pharmacokinetic studies. Felbamate-d5 is valuable in research applications pertaining to epilepsy, neuronal excitability, and NMDA receptor modulation.

Orphenadrine-d3 hydrochloride is a deuterium-labeled form of Orphenadrine hydrochloride, serving as a stable isotope for research applications. It acts as a non-competitive antagonist of the NMDA receptor, effectively crossing the blood-brain barrier, with a Ki value of 6.0 μM. This compound is primarily utilized in studies exploring its analgesic effects for muscle stiffness, pain, and discomfort, and is also relevant in research on neurodegenerative diseases and the management of tremors associated with Parkinson's disease. Its neuroprotective properties make it a valuable tool in the investigation of various central nervous system disorders.

Piracetam-d8 is a deuterium-labeled analog of Piracetam, a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA). This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research, facilitating the investigation of Piracetam's role in cognitive enhancement and treatment of cognitive disorders. Its unique labeling allows for precise tracking of metabolic pathways and interactions in biological systems.