Isotope-Labeled Compounds

Items 3701-3750 of 7447

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  1. Stable Isotope

    6-Aminocaproic acid-d10 hydrochloride is a deuterium-labeled derivative of 6-Aminocaproic acid, a potent antifibrinolytic agent that targets plasmin and plasminogen. By competitively binding to lysine residues on plasminogen, it effectively inhibits the formation of plasmin, thereby preventing clot lysis and reducing fibrinolytic activity. This reagent is valuable for research applications focused on bleeding disorders and related therapeutic interventions.
  2. Stable Isotope

    Dicoumarol-d8 is a deuterated form of Dicoumarol, targeting NAD(P)H:quinone oxidoreductase 1 (NQO1) and pyruvate dehydrogenase kinase 1 (PDK1). It exhibits inhibitory activity with IC50 values of 0.37 μM for NQO1 and 19.42 μM for PDK1. This stable isotope-labeled reagent is valuable in biochemical research and metabolic studies, providing insights into enzyme function and regulation.
  3. Stable Isotope

    Metaxalone-d3 is a deuterium-labeled form of Metaxalone, an FDA-approved muscle relaxant primarily acting on the central nervous system. Its primary mechanism involves inhibition of polysynaptic reflex arcs, promoting muscle relaxation. Additionally, Metaxalone demonstrates inhibitory effects on MAO-A, contributing to its anti-inflammatory and antioxidant properties. This reagent is useful for research applications investigating inflammatory responses, as it modulation of IL-1β-induced phenotypes impacts NF-κB and related signaling pathways in microglia.
  4. Stable Isotope

    Metaxalone-d6 is a deuterium-labeled analog of Metaxalone, an FDA-approved muscle relaxant primarily targeting the central nervous system. It promotes muscle relaxation by inhibiting polysynaptic reflex arcs and also exhibits activity as an inhibitor of MAO-A, contributing to anti-inflammatory and antioxidant effects. Metaxalone effectively reduces the IL-1β-induced inflammatory phenotype, modulates NF-κB signaling pathways, and lowers both expression and activity of MAO-A in IL-1β-treated microglia, making it a valuable tool for research in neurobiology and inflammation.
  5. Stable Isotope

    Varespladib-d7 is a deuterated derivative of Varespladib, a selective inhibitor of group IIA secretory phospholipase A2 (sPLA2) with an IC50 of 9 nM. This reagent effectively inhibits sPLA2 activity across serum samples from multiple species, demonstrating IC50 values of 8.1 nM in rats, 5.0 nM in rabbits, 3.2 nM in guinea pigs, and 6.2 nM in humans. Varespladib-d7 serves as a valuable tool in pharmacokinetic studies and metabolic research involving sPLA2 pathways.
  6. Stable Isotope

    Triethylene glycol-d12 is a deuterium-labeled form of triethylene glycol, serving as a stable isotope for various research applications. This PEG-based linker facilitates the synthesis of PROTACs, enabling targeted protein degradation. Its unique isotopic labeling allows for enhanced tracking and characterization in biochemical studies, making it a valuable reagent for researchers focused on protein targeting and modulation.
  7. Stable Isotope

    NH2-C4-NH-Boc-d8 is a deuterated PROTAC linker that facilitates the design of targeted protein degradation systems. This compound connects two distinct ligands: one that targets an E3 ubiquitin ligase and another that binds the protein of interest. It is valuable for synthesizing a range of PROTACs that utilize the ubiquitin-proteasome pathway to selectively degrade specific proteins, making it a key tool in chemical biology and therapeutic development.
  8. Isotope-Labeled Compound

    O,O-Dimethyl dithiophosphate-13C2 ammonium is an isotope-labeled compound, specifically the 13C variant of O,O-Dimethyl dithiophosphate ammonium. This reagent is utilized in various research applications, including metabolic studies and tracer experiments, to facilitate the investigation of biochemical pathways and enzyme kinetics. Its isotopic labeling allows for enhanced detection and quantification in mass spectrometry analyses, contributing to a deeper understanding of molecular interactions.
  9. Stable Isotope

    Enzalutamide-d6 is a deuterium-labeled version of the androgen receptor antagonist Enzalutamide (MDV3100). This stable isotope is utilized in research to trace metabolic pathways and study the pharmacokinetics of AR-targeted therapies. With an IC50 of 36 nM in LNCaP prostate cancer cells, Enzalutamide serves a critical role in prostate cancer research and drug development.
  10. Stable Isotope

    Darolutamide-d4 is a deuterium-labeled analog of Darolutamide, a competitive androgen receptor (AR) antagonist. It demonstrates a Ki of 11 nM for rat wild-type AR and an IC50 of 26 nM for human wild-type AR-mediated transcriptional activation, effectively inhibiting testosterone-induced AR nuclear translocation. This reagent selectively impacts AR-positive cells by disrupting AR-dependent signaling pathways, while its active metabolite retains full antagonistic activity against AR mutants. Darolutamide-d4 is valuable for research into prostate cancer, particularly in studies focused on androgen receptor-dependent mechanisms.
  11. Stable Isotope

    11-Ketodihydrotestosterone-d3 is a deuterium-labeled derivative of 11-Ketodihydrotestosterone, an endogenous steroid and active androgen. This compound acts as a potent agonist of the androgen receptor (AR), exhibiting a Ki value of 20.4 nM and an EC50 of 1.35 nM for human AR. It plays a significant role in the regulation of gene expression, protein synthesis, and cell proliferation in androgen-dependent prostate cancer research. 11-Ketodihydrotestosterone-d3 is valuable for metabolic studies and tracer applications in hormonal and cancer research.
  12. Stable Isotope

    Linuron-d6 is a deuterated form of the phenylurea herbicide Linuron, which functions as a photosystem II inhibitor. This compound is primarily utilized in agricultural settings to effectively manage the growth of grass and weeds in crops and orchards. In addition to its herbicidal properties, Linuron exhibits activity as a competitive antagonist of the androgen receptor, with a Ki of 100 μM, and has been shown to induce reproductive toxicity in animal models, acting as an endocrine disruptor in research contexts.
  13. Stable Isotope

    Apalutamide-d3 is a deuterium-labeled derivative of Apalutamide, a highly selective androgen receptor (AR) antagonist with an IC50 of 16 nM. This stable isotope is designed for applications in pharmacokinetic studies and metabolic profiling, facilitating the investigation of AR signaling pathways and the pharmacodynamics of AR-targeted therapies in various models. Its use in research enables precise tracking and quantification in biological systems, enhancing our understanding of androgen receptor modulation in cancer therapies.
  14. Stable Isotope

    Ostarine-d4 is a deuterated form of Ostarine, primarily functioning as a stable isotope. This labeled compound is utilized in pharmacokinetic studies, enabling accurate tracking of Ostarine metabolism and distribution within biological systems. Its application is critical for research on selective androgen receptor modulators and their effects on muscle and bone metabolism.
  15. Stable Isotope

    Nilutamide-d6 is a deuterium-labeled derivative of Nilutamide, a non-steroidal anti-androgen agent primarily targeting androgen receptors. This stable isotope is utilized in metabolic studies and pharmacokinetic research of Nilutamide, particularly in the context of metastatic prostate carcinoma. Its precise labeling allows for enhanced tracking and quantification of drug metabolism and efficacy in various biological systems.
  16. Stable Isotope

    Flutamide-d7 is a deuterated form of Flutamide, serving as a stable isotope used in metabolic and pharmacokinetic studies. This compound is instrumental in tracing the metabolic pathways of Flutamide, enhancing the understanding of its pharmacodynamics and pharmacokinetics. Flutamide-d7 is primarily applied in research focused on androgen receptor modulation and anti-androgen therapies.
  17. Stable Isotope

    Cyproterone acetate-d3 is a deuterated form of Cyproterone acetate, a synthetic steroid exhibiting anti-androgenic and progestogenic activities. It demonstrates an IC50 of 7.1 nM and binds selectively to progesterone and glucocorticoid receptors. This stable isotope is valuable for research applications involving hormonal regulation, receptor signaling studies, and metabolic pathway investigations involving steroid hormones.
  18. Stable Isotope

    Boc-Glycine-2-13C is a stable isotope-labeled derivative of Boc-Glycine. This compound serves as a valuable tool in metabolic labeling studies and isotopic tracing experiments. Its incorporation into biomolecular studies enables precise quantitative analysis in various research applications, including protein synthesis and metabolic pathways in cellular systems.
  19. Stable Isotope

    Ketodarolutamide-d3 is a deuterium-labeled derivative of Ketodarolutamide, a potent and high-affinity nonsteroidal androgen receptor (AR) antagonist. It exhibits a Ki value of 8 nM for rat wild-type AR and an IC50 of 38 nM in AR-HEK293 cells, effectively inhibiting testosterone-induced nuclear translocation of the AR. This compound specifically suppresses the proliferation of AR-dependent prostate cancer cells and demonstrates antitumor activity in models of castration-resistant prostate cancer (CRPC). Ketodarolutamide-d3 is a valuable tool for mechanistic and therapeutic research in prostate cancer studies.
  20. Stable Isotope

    Diethylstilbestrol-d8 is a deuterated form of Diethylstilbestrol, a synthetic nonsteroidal estrogen. It primarily targets estrogen receptors and is utilized in research to study the pharmacokinetics and metabolic pathways of estrogens. This stable isotope-labeled compound is essential for investigations into estrogen-related disorders and the physiological effects of estrogenic compounds.
  21. Stable Isotope

    4-Nonylphenol-d5 is the deuterated form of 4-Nonylphenol, serving as a stable isotope for analytical applications. As a significant breakdown product of Nonylphenol ethoxylates (NPEOs), it is recognized for its persistence in the environment and its endocrine-disrupting effects, exhibiting estrogenic activity. This reagent is valuable in studies examining environmental contamination, toxicology, and endocrine disruption pathways.
  22. Stable Isotope

    Monoethyl fumarate-d5 is a deuterium-labeled derivative of monoethyl fumarate, functioning as a stable isotope standard in research applications. It primarily activates the Nrf2 pathway, playing a crucial role in cellular defense mechanisms against oxidative stress. Additionally, monoethyl fumarate serves as an effective preservative and polymerization agent for macromolecular materials, making it valuable in various biochemical and pharmaceutical studies.
  23. Stable Isotope

    (R)-(-)-Ibuprofen-d3 is a deuterium-labeled derivative of the R enantiomer of Ibuprofen. This compound is utilized as a stable isotope in pharmacokinetic and metabolic studies. While the (R)-(-)-Ibuprofen itself is inactive on COX and inhibits NF-κB activation, it is recognized for its anti-inflammatory and antinociceptive properties, making this isotope valuable for research applications focused on drug metabolism and efficacy.
  24. Isotope-Labeled Compound

    Pyridoxine-d3 is a deuterium-labeled derivative of pyridoxine (vitamin B6), primarily used as an isotope-labeled compound for metabolic research. It exhibits antioxidant properties in cellular models of Alzheimer's disease through modulation of the Nrf2/HO-1 signaling pathway. Pyridoxine-d3 serves as a valuable tool in studying vitamin B6 metabolism and its neuroprotective roles in neurodegenerative conditions, facilitating the understanding of its biochemical mechanisms.
  25. Stable Isotope

    Geranylgeraniol-d5 is a deuterated form of geranylgeraniol, which serves as a stable isotope. As an orally active vitamin K2 subtype and an intermediate in the mevalonate pathway, geranylgeraniol primarily targets the NF-kB signaling pathway. Research has demonstrated its potential to alleviate LPS-induced microglial inflammation in animal models, making it a valuable compound for studies focused on inflammatory responses and neurobiology.
  26. Stable Isotope

    TML-6-d3 is a deuterated derivative of the curcumin compound TML-6, demonstrating stability as a labeled isotope. This reagent primarily inhibits the synthesis of β-amyloid precursor protein and β-amyloid (Aβ), contributing to research in neurodegenerative diseases. TML-6-d3 upregulates ApoE, suppresses NF-κB and mTOR signaling pathways, and enhances activities related to neuroprotection. It serves as a valuable tool for studying the molecular mechanisms of Alzheimer's disease and related disorders.
  27. Stable Isotope

    Scyllo-Inositol-d6 is a deuterium-labeled version of Scyllo-Inositol that serves as a stable isotope. This compound acts as an inhibitor targeting the aggregation of misfolded proteins, including α-synuclein and Amyloid-β, effectively crossing the blood-brain barrier. Scyllo-Inositol-d6 selectively binds to and stabilizes non-toxic oligomers, preventing their transformation into harmful aggregates while enhancing mechanisms of protein homeostasis and neuroprotection. It is valuable in research related to neurodegenerative diseases, such as Parkinson's disease, Alzheimer's disease, and Huntington's disease.
  28. Stable Isotope

    Glimepiride-d8 is a deuterium-labeled analog of Glimepiride, which primarily targets the sulfonylurea receptor. This stable isotope is utilized in pharmacokinetic studies, allowing for the accurate tracking of drug metabolism and disposition in biological systems. It serves as a valuable tool in research involving diabetes treatment and the investigation of metabolic pathways.
  29. Stable Isotope

    Glimepiride-d4-1 is a deuterium-labeled version of Glimepiride, a medium-to-long acting sulfonylurea antidiabetic agent. This stable isotope is utilized for metabolic studies and pharmacokinetic research, providing insight into the drug's bioavailability and mechanism of action. The compound is valuable in assessing the therapeutic potential and safety profiles of Glimepiride in diabetes management.
  30. Stable Isotope

    Methyl tridecanoate-d25 is a deuterium-labeled derivative of methyl tridecanoate, functioning as a stable isotope. This compound exhibits moderate inhibition of β-amyloid aggregation, making it relevant for studies related to neurodegenerative diseases. Additionally, it shows weak inhibition of acetylcholinesterase (AChE), offering potential applications in enzyme activity assays and the investigation of cholinergic signaling.
  31. Stable Isotope

    Glimepiride-d4-2 is a deuterium-labeled derivative of Glimepiride, a medium-to-long acting sulfonylurea used primarily in the management of type 2 diabetes mellitus. This compound acts by enhancing insulin secretion from pancreatic beta cells, thereby lowering blood glucose levels. Glimepiride-d4-2 is utilized in pharmacokinetic studies and metabolic research to understand the drug's behavior and efficacy in biological systems.
  32. Stable Isotope

    Choline-d4 chloride is a stable isotope of choline chloride, a quaternary ammonium salt that acts as an acyl group acceptor and a substrate for choline acetyltransferase. This compound plays a critical role in various biological processes, including neurotransmitter synthesis and lipid metabolism. Research applications of Choline-d4 chloride include metabolic studies, tracer experiments, and investigations into choline's role in growth and development, particularly in animal nutrition.
  33. Stable Isotope

    Choline-d9 chloride is a deuterium-labeled form of choline chloride, classified as a quaternary ammonium salt. It serves as a substrate for choline acetyltransferase and acts as an acyl group acceptor, making it valuable in various biochemical assays. This stable isotope is particularly useful in metabolic studies and tracer experiments, providing insights into choline metabolism and its physiological roles. In addition, it is important as a nutritional supplement in animal feed, especially in promoting growth in poultry.
  34. Stable Isotope

    Pyridostigmine-d6 bromide is a deuterated form of Pyridostigmine, functioning as a reversible cholinesterase inhibitor and parasympathomimetic agent. This stable isotope is useful for metabolic studies and tracking the pharmacokinetics of drugs in biological systems. Its labeling with deuterium allows for enhanced precision in mass spectrometry applications and other analytical techniques in chemical research.
  35. Stable Isotope

    Chlorpyrifos-d10 is a deuterium-labeled variant of Chlorpyrifos, an organophosphate insecticide known for its action as a phosphorothionate. Its active metabolite, Chlorpyrifos oxon, functions as a potent inhibitor of acetylcholinesterase (AChE), thereby disrupting neurological function in a range of organisms, including insects and mammals. This stable isotope is valuable for studying metabolic pathways, neurotoxic effects, and enzyme interactions, particularly in the context of susceptibility to neurotoxicity modulated by plasma enzyme paraoxonase 1 (PON1).
  36. Stable Isotope

    4-Methylbenzylidene camphor-d4 is a deuterated stable isotope of 4-Methylbenzylidene camphor, a compound widely studied for its applications in photoprotection. This labeled compound serves as a valuable tool for tracing and quantifying chemical interactions in biological systems. It is particularly useful in research involving sunscreen formulation studies and the investigation of UV-absorbing properties in various matrices.
  37. Stable Isotope

    Donepezil-d5 hydrochloride is a stable deuterium-labeled analogue of Donepezil, which acts as a reversible and selective inhibitor of acetylcholinesterase (AChE) with an IC50 value of 6.7 nM. Its high selectivity for AChE over butyrylcholinesterase (BuChE) makes it a valuable tool in studying cholinergic signaling. Donepezil-d5 also demonstrates neuroprotective effects against Aβ42-induced neurotoxicity, making it relevant in Alzheimer's disease research and other neurodegenerative studies.
  38. Stable Isotope

    Donepezil-d5 is a deuterium-labeled form of Donepezil, a potent and selective inhibitor of acetylcholinesterase (AChE). It demonstrates inhibitory activities with IC50 values of 8.12 nM for bovine AChE and 11.6 nM for human AChE. This stable isotope is valuable for pharmacokinetic studies and metabolic profiling in research related to neurodegenerative diseases, particularly Alzheimer's disease.
  39. Stable Isotope

    Physostigmine-d3 is the deuterated form of Physostigmine, a reversible inhibitor of acetylcholinesterase (AChE). This compound effectively crosses the blood-brain barrier, enhancing central cholinergic neurotransmission, and is utilized in research for its ability to reverse memory deficits in transgenic mouse models of Alzheimer's disease. Additionally, Physostigmine serves as an antidote for anticholinergic poisoning, making it significant for studies in neuropharmacology and toxicology.
  40. Stable Isotope

    Donepezil-d7 hydrochloride is a deuterium-labeled variant of Donepezil, a potent inhibitor of acetylcholinesterase (AChE). This compound exhibits specific inhibition with IC50 values of 8.12 nM for bovine AChE and 11.6 nM for human AChE. Donepezil-d7 hydrochloride is primarily used in chemical research to trace the metabolism and pharmacokinetics of Donepezil in various biological systems.
  41. Stable Isotope

    Chlorpyrifos-oxon-d10 is a deuterium-labeled derivative of Chlorpyrifos-oxon, which serves as a potent inhibitor of acetylcholinesterase (AChE) through phosphorylating action. This compound has been shown to induce cross-linking between tubulin subunits, thereby disrupting microtubule dynamics and function. Its use in research applications includes studying the mechanisms of neurotoxicity and the evaluation of pesticide metabolism.
  42. Stable Isotope

    Profenofos-d3 is a stable isotope-labeled derivative of Profenofos, an insecticide known for its application in field crops, vegetables, and fruit crops. It functions as an acetylcholinesterase (AChE) inhibitor, exhibiting neurotoxic effects that can impact insect populations. This reagent is valuable for research applications involving pharmacokinetics and metabolic studies of insecticides, enabling precise tracking in biological systems.
  43. Stable Isotope

    Acephate-d3 is a deuterated analogue of Acephate, serving as a stable isotope. This compound primarily acts as an anticholinesterase insecticide, exhibiting cholinotoxic effects. While it demonstrates weak inhibition of rat acetylcholinesterase (AChE), it exhibits potent inhibition of AChE in cockroaches, making it valuable for research in insect physiology and pest management studies.
  44. Stable Isotope

    Donepezil-d4 hydrochloride is a deuterium-labeled derivative of Donepezil hydrochloride, a reversible and selective inhibitor of acetylcholinesterase (AChE) with an IC50 of 6.7 nM. This compound demonstrates a strong selectivity for AChE over butyrylcholinesterase (BuChE) and exhibits neuroprotective effects against Aβ42-induced neurotoxicity. Donepezil-d4 is valuable for studying AChE interactions and pharmacokinetics in neurodegenerative disease research.
  45. Stable Isotope

    Azamethiphos-d6 is a deuterated form of Azamethiphos, an organophosphate insecticide that primarily targets acetylcholinesterase (AChE). This compound is effectively used in research to study the inhibition of AChE activities and its implications in controlling sea lice populations. Azamethiphos-d6 serves as a valuable stable isotope for analytical studies and environmental monitoring of organophosphate residues.
  46. Stable Isotope

    (Rac)-Rivastigmine-d6 is a stable isotope-labeled form of Rivastigmine, a potent inhibitor of cholinesterases, specifically butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), with IC50 values of 0.037 μM and 4.15 μM, respectively. This compound effectively crosses the blood-brain barrier, making it a valuable tool for investigating cholinergic mechanisms.(Rac)-Rivastigmine-d6 is primarily utilized in research focused on mild to moderate Alzheimer's dementia and dementia associated with Parkinson's disease, facilitating studies on neurotransmission and therapeutic interventions.
  47. Stable Isotope

    Acephate-d6 is a deuterium-labeled derivative of Acephate, a widely used anticholinesterase insecticide. It functions by inhibiting acetylcholinesterase (AChE) activity in insects, leading to disruption of their nervous system and effective pest control. This stable isotope variant is useful for research applications involving metabolic studies, pesticide residue analysis, and environmental monitoring in agricultural and horticultural settings.
  48. Stable Isotope

    Protriptyline (N-methyl-d3) hydrochloride is a deuterium-labeled derivative of the tricyclic antidepressant protriptyline, primarily targeting noradrenergic and serotonergic pathways. This compound exhibits key biological activities such as enhancing wakefulness, making it beneficial for research in sleep disorders like narcolepsy, as well as in studies related to depression and attention deficit hyperactivity disorder (ADHD). Its energizing effects distinguish it from other tricyclic antidepressants, providing valuable insights into the pharmacological profiles of psychiatric treatments.
  49. Stable Isotope

    Donepezil-d7 is a deuterium-labeled analog of Donepezil, a selective and potent inhibitor of acetylcholinesterase (AChE). This compound demonstrates impressive inhibitory activity with IC50 values of 8.12 nM for bovine AChE and 11.6 nM for human AChE, making it a valuable tool for studying cholinergic signaling and Alzheimer's disease. Researchers can utilize Donepezil-d7 in pharmacokinetic studies and metabolic profiling to better understand the compound's activity and metabolism in various biological contexts.
  50. Stable Isotope

    Desipramine-d4 is a deuterium-labeled derivative of Desipramine, primarily serving as a stable isotope for various analytical applications. This compound is utilized in pharmacokinetic studies and metabolic research to trace the behavior of Desipramine in biological systems. It aids in enhancing the accuracy of quantification methods in mass spectrometry and other analytical techniques.

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