Isotope-Labeled Compounds

p,p'-DDD-13C12 is a stable isotope-labeled form of p,p'-DDD, a primary metabolite of p,p'-DDT. This compound is valuable for tracking metabolic pathways and biotransformation studies in research involving halogenated insecticides. Its presence can be analyzed in biological samples, such as feces and liver tissues, to better understand the pharmacokinetics and toxicokinetics of p,p'-DDT exposure in experimental models.

Lovastatin-d3 hydroxy acid sodium is a deuterium-labeled derivative of Lovastatin hydroxy acid sodium, a potent inhibitor of HMG-CoA reductase, with a Ki of 0.6 nM. This stable isotope is utilized in metabolic studies to investigate cholesterol biosynthesis and regulation. It serves as a valuable tool for researchers examining the pharmacokinetics and pharmacodynamics of statins in biochemical and clinical research applications.

IDO-IN-7-d10 is a deuterium-labeled analogue of IDO-IN-7, a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with an IC50 value of 38 nM. This stable isotope derivative is designed for use in metabolic studies and biomarker analysis, enhancing the understanding of IDO1-related pathways in cancer and immune response research. Its use in tracer studies allows for improved tracking of metabolic processes.

(S)-Indoximod-d3 is a deuterium-labeled form of (S)-Indoximod, an inhibitor of indoleamine 2,3-dioxygenase (IDO). This stable isotope retains the biological activity of the parent compound, allowing for precise tracking and measurement in metabolic studies. (S)-Indoximod-d3 is primarily utilized in cancer research, particularly in studies exploring immune modulation and tumor microenvironment interactions.

IDH1 Inhibitor 7-d2 is a deuterium-labeled derivative of IDH1 Inhibitor 7, targeting the isocitrate dehydrogenase 1 (IDH1) enzyme. It exhibits potent inhibitory activity with an IC50 of less than 100 nM. This stable isotope-labeled compound serves as a valuable tool for in vivo and in vitro studies aimed at investigating IDH1-related metabolic pathways and the development of targeted cancer therapies.

Enasidenib-d6 is a deuterated analogue of Enasidenib, a potent, reversible inhibitor selectively targeting mutant IDH2 enzymes. It exhibits IC50 values of 100 nM for IDH2R140Q and 400 nM for IDH2R172K, demonstrating significant biological activity in modulating the pathways associated with these mutations. This stable isotope-labeled compound is useful in research applications such as metabolic studies, pharmacokinetic profiling, and elucidation of IDH2-related cellular mechanisms.

Hexane-1,6-diol-d4 is a deuterated stable isotope form of Hexane-1,6-diol, a six-carbon straight-chain diol characterized by hydroxyl groups at each end. This reagent serves as a valuable additive in drilling fluids and is also utilized as a substrate in various life science research applications. Its stable isotope labeling facilitates the tracking of metabolic pathways and enhances the understanding of biochemical processes.

DSPC-d70, or 1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d70, is a deuterium-labeled lipid that serves as a cylindrical-shaped phospholipid. It is primarily utilized in the formation of liposomes and acts as a key component in lipid nanoparticle (LNP) systems. DSPC-d70 is beneficial for studying lipid dynamics and membrane interactions, particularly in drug delivery and nanomedicine research applications.

DSPC-d83 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83) is a deuterium-labeled derivative of DSPC, a cylindrical-shaped phospholipid. This reagent is crucial for the synthesis of liposomes and serves as a key lipid component in lipid nanoparticle (LNP) formulations. Its stable isotope labeling facilitates tracking and characterization in biological research, making it valuable for studies involving drug delivery and membrane dynamics.

DSPC-d4 (1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d4) is a deuterium-labeled derivative of DSPC, a cylindrical-shaped phospholipid. This reagent is crucial for the synthesis of liposomes and functions as a key lipid component in lipid nanoparticle (LNP) formulations. DSPC-d4 is utilized in various biological applications, including drug delivery research and the study of membrane dynamics, contributing valuable insights into lipid biology and nanotechnology.

Dantrolene-13C3 is a stable isotope-labeled analog of Dantrolene, a muscle relaxant that non-competitively inhibits human erythrocyte glutathione reductase, with Ki and IC50 values of 111.6 μM and 52.3 μM, respectively. As a ryanodine receptor antagonist, Dantrolene-13C3 plays a critical role in stabilizing Ca2+ signaling. This reagent is suitable for research applications related to muscle spasticity, malignant hyperthermia, Huntington's disease, and neuroleptic malignant syndrome.

Migalastat hydrochloride-15N is a stable isotope-labeled form of Migalastat hydrochloride, an orally active molecular chaperone targeting α-galactosidase A. It exhibits a potent IC50 of 0.04 μM for human α-Gal A, facilitating the proper folding and lysosomal transport of certain unstable mutant forms of the enzyme. Upon dissociation in the acidic lysosomal environment, Migalastat promotes restoration of biological activity, making it valuable for research in lysosomal storage disorders and enzyme replacement therapies.

Acarbose-d4 is a deuterium-labeled derivative of Acarbose, targeting alpha-glucosidases. This stable isotope maintains the biological activity of its parent compound, functioning as an antihyperglycemic agent with an IC50 of 11 nM. Acarbose-d4 is utilized in research to study glucose metabolism and the enhancement of hypoglycemic effects in combination therapies involving sulfonylureas or insulin.

S-Sulfo-DL-cysteine-d3 is a stable isotope-labeled analog of S-Sulfo-DL-cysteine featuring deuterium at the 2, 3, and 3 positions. This compound is utilized in metabolic studies and isotopic tracing experiments, allowing for precise analysis of cysteine metabolism and biochemical pathways. Its deuterium labeling provides a valuable tool for researchers pursuing kinetic and mechanistic investigations in various biological systems.

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.

Tetrabenazine-d7 is a deuterium-labeled derivative of Tetrabenazine, a reversible inhibitor of the vesicular monoamine transporter VMAT2, demonstrating a Kd value of 1.34 nM. This compound is essential in biochemical research focused on hyperkinetic movement disorders, including Huntington's disease. The stable isotope labeling allows for enhanced tracking and analysis in metabolic studies and pharmacokinetic evaluations.

α-Cyano-4-hydroxycinnamic acid-d4 is a deuterium-labeled derivative of α-Cyano-4-hydroxycinnamic acid, which acts as a non-competitive inhibitor of monocarboxylate transporters (MCTs). It effectively inhibits the mitochondrial pyruvate transporter with a Ki value of 6.3 μM. This stable isotope is widely utilized as a matrix to enhance peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications, aiding in the analysis and characterization of biomolecules.

Prilocaine Hydrochloride-d7 is a deuterium-labeled derivative of prilocaine hydrochloride, functioning as a stable isotope. This amino amide compound acts as an inhibitor of Na/K-ATPase, exhibiting neurotoxic effects that are relevant in neuroscientific research. Its isotopic labeling allows for precise tracking and analysis in pharmacokinetic studies and metabolic profiling.

Choline-13C2 chloride is a stable isotope-labeled form of choline chloride, an essential nutrient implicated in various biological processes. Its primary mechanism involves the activation of alpha7 nicotinic receptors, contributing to analgesic and anti-inflammatory effects. This compound is utilized in research applications related to liver disease, atherosclerosis, and neurological disorders, facilitating studies that require isotope tracing and metabolic analysis.

(Rac)-Monepantel sulfone-d5 is a deuterium-labeled variant of Monepantel, an organic anthelmintic agent. It functions as a positive allosteric modulator of nematode-specific nicotinic acetylcholine receptor (nAChR) subunits, enhancing receptor activity. This stable isotope is valuable for research applications in studying nematode physiology and drug interaction mechanisms.

(Rac)-Monepantel-d5 is a deuterium-labeled derivative of Monepantel, an organic anthelmintic. It functions as a positive allosteric modulator of nematode-specific nicotinic acetylcholine receptor (nAChR) subunits, enhancing receptor activity. This reagent is valuable for research applications in parasitology and neurobiology, facilitating studies on receptor modulation and nematode physiology.

Myosmine-d4 is a deuterated form of myosmine, a tobacco alkaloid known for its role in various biological systems. It exhibits low affinity for the α4β2 nicotinic acetylcholinergic receptors (nAChR), with a Ki of 3300 nM. This stable isotope is primarily used in pharmacokinetic studies and metabolic labeling experiments, providing valuable insights into the behavior and fate of myosmine in biological matrices.

Flupyradifurone-d5 is a deuterated derivative of Flupyradifurone, a systemic nicotinic acetylcholine receptor (nAChR) agonist. This compound disrupts signal transduction in the central nervous system of sucking pests, making it effective as a butenolide insecticide. Flupyradifurone-d5 can be utilized in research focused on pest control mechanisms and the study of insecticide efficacy in agricultural applications.

Anabaseine-d4 is a deuterium-labeled form of Anabaseine, functioning as a non-selective nicotinic receptor agonist. This compound effectively stimulates all acetylcholine receptors (AChRs), with a particular preference for skeletal muscle and brain α7 subtypes. Additionally, Anabaseine exhibits weak partial agonistic activity at α4β2 nAChRs, making it valuable for research applications focused on neurotransmission and neuromuscular function.

Varenicline-15N3 Hydrochloride is the nitrogen-15 labeled isotope of Varenicline hydrochloride, a known partial agonist of the α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) with an IC50 value of 250 nM. It targets nicotine dependence by mitigating the direct agonistic effects of nicotine while providing moderate stimulation of nAChR. Additionally, Varenicline exhibits partial agonist activity at α6β2 nAChR and full agonism at another subset of this receptor. This isotope-labeled compound is valuable for pharmacokinetic studies and research into nicotine addiction and smoking cessation therapies.

Cytisine-d4 is a deuterium-labeled derivative of Cytisinicline, an alkaloid known for its role as a partial agonist at α4β2 nicotinic acetylcholine receptors (nAChRs) and for displaying full to partial agonism at β4-containing and α7 receptors. This stable isotope is utilized in research applications aimed at studying receptor interactions and pharmacokinetics, as well as in investigations related to smoking cessation therapies. The incorporation of deuterium allows for enhanced tracking of metabolic pathways and biological activity in various experimental settings.

Varenicline-d4 is a deuterium-labeled derivative of Varenicline, a potent partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Additionally, Varenicline acts as a full agonist at the α3β4 and α7 nAChRs, exhibiting EC50 values of 55 μM and 18 μM, respectively. This stable isotope is instrumental for research involving smoking cessation therapies and the pharmacological investigation of nicotinic receptors.

Mecamylamine-d3 hydrochloride is a deuterium-labeled derivative of Mecamylamine hydrochloride, functioning as a nonselective, noncompetitive antagonist of nicotinic acetylcholine receptors (nAChR). This stable isotope is employed in research applications focused on neuropsychiatric disorders and the pharmacological assessment of nAChR activity. Its ability to cross the blood-brain barrier facilitates investigations into central nervous system functions and disorders, as well as potential therapeutic interventions.

Varenicline-13C,15N is a stable isotope-labeled variant of Varenicline, a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR), with an IC50 of 250 nM. This compound also interacts with α6β2 nAChR as a partial agonist and activates α7β2 nAChR as a full agonist. Varenicline-13C,15N is utilized in research to study nicotine dependence and the pharmacodynamics of smoking cessation therapies, providing valuable insights into receptor interactions and metabolic pathways.

Bendroflumethiazide-d5 is a deuterium-labeled derivative of Bendroflumethiazide, functioning primarily as a diuretic. It acts by inhibiting the electroneutral sodium-chloride symporter located in the apical membrane of the distal convoluted tubule, which contributes to its ability to lower blood pressure. This reagent is valuable for research applications involving hypertension, edema, and the evaluation of antidiuretic effects in conditions such as diabetes insipidus. Its stable isotope format supports precise tracing and metabolic studies.

Bumetanide-d5 Butyl Ester is a deuterium-labeled derivative of Bumetanide Butyl Ester, designed as a stable isotope for analytical research. It is primarily utilized in mass spectrometry applications to trace metabolic pathways and pharmacokinetics. This reagent aids in understanding the biological activity of Bumetanide and its effects on ion transport mechanisms, making it an essential tool for drug development and pharmacological studies.

Lesinurad-d4 is a deuterium-labeled derivative of Lesinurad, primarily targeting URAT1 and OAT transporters. This stable isotope can aid in the pharmacokinetic profiling of Lesinurad by facilitating quantification in biological samples. Research applications include studies on uric acid handling in the kidney and the exploration of drug transporter interactions, contributing to a deeper understanding of renal pharmacology.

Tezacaftor-d6 is a deuterium-labeled variant of Tezacaftor, a CFTR corrector designed to facilitate the proper trafficking of the F508del CFTR protein to the cell surface. Its primary mechanism involves correcting defects associated with cystic fibrosis (CF), particularly in patients homozygous for the CFTR Phe508del mutation. While Tezacaftor enhances CFTR protein presence, the co-administration with Ivacaftor, a CFTR potentiator, further improves channel activity, demonstrating significant therapeutic potential. This reagent is essential for studying CFTR modulation and the development of combination therapies for cystic fibrosis management.

Niflumic acid-13C6 is a stable isotope-labeled derivative of Niflumic acid, a selective blocker of Ca2+-activated Cl- channels. It exhibits analgesic and anti-inflammatory properties, making it relevant in the treatment of conditions such as rheumatoid arthritis. This labeled compound is primarily utilized in metabolic studies and kinetics research, enabling detailed investigations into drug metabolism and pharmacokinetics.