Isotope-Labeled Compounds

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  1. Stable Isotope

    Sacubitril-d4 is a deuterated form of Sacubitril, a selective neprilysin (NEP) inhibitor with an IC50 value of 5 nM. This stable isotope is utilized in analytical studies to trace metabolic pathways and pharmacokinetics related to heart failure therapies, particularly those involving the combination treatment LCZ696. Researchers can employ Sacubitril-d4 to investigate its biochemical profiles and interaction dynamics in various biological systems.
  2. Stable Isotope

    Racecadotril-d5 is a deuterated form of Racecadotril, a neutral endopeptidase (NEP) inhibitor. It exhibits significant inhibition of NEP activity in mouse brain tissues, with reported inhibition constants (Kis) of 4500 nM for Racecadotril and 6.1 nM for its active metabolite, Thiorphan. Racecadotril-d5 serves as a valuable tool for research applications involving pain modulation and gastrointestinal studies, further contributing to the understanding of NEP's role in various biological processes.
  3. Stable Isotope

    Thiorphan-d7 is a deuterium-labeled derivative of Thiorphan, a selective inhibitor of neprilysin (NEP) with an IC50 value of 6.9 nM. This stable isotope-labeled compound enables advanced metabolic studies and tracking of NEP-related pathways in various biological contexts. Thiorphan-d7 is valuable for research applications involving the modulation of neuropeptide levels and the investigation of neurodegenerative diseases.
  4. Stable Isotope

    Thiorphan-d5 is a deuterated form of Thiorphan, a well-known inhibitor of the enkephalin-degrading enzyme, neprilysin. This stable isotope-labeled compound is utilized in pharmacokinetic studies and metabolic profiling, providing valuable insights into drug metabolism and efficacy. It serves as an essential tool for researchers investigating neuropeptide regulation and pain modulation in biochemical assays.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. Stable Isotope

    Saflufenacil-d7 is a deuterium-labeled variant of Saflufenacil, a herbicide belonging to the pyrimidinedione class. This compound acts as a potent inhibitor of protoporphyrinogen IX oxidase (PPO), providing effective preplant burndown and selective preemergence control of dicot weeds in various crops, including corn. Saflufenacil-d7 is primarily utilized in chemical research for tracking and understanding the behavior of Saflufenacil in biological systems and environmental studies.
  11. Stable Isotope

    AGN 193109-d7 is a deuterated variant of AGN 193109, a retinoid analog that serves as a potent and selective antagonist of retinoic acid receptors (RARs). It exhibits strong binding affinities with Kd values of 2 nM for RARα, 2 nM for RARβ, and 3 nM for RARγ. This stable isotope is valuable for research applications involving the investigation of RAR-mediated pathways and the effects of retinoid signaling in various biological contexts.
  12. Stable Isotope

    L-Azidohomoalanine-1,2,3,4-13C4 hydrochloride is a stable isotope-labeled variant of L-Azidohomoalanine, featuring both 13C and 15N isotopes. This reagent acts as a versatile PROTAC linker, facilitating the synthesis of protein-targeting chimeras. It serves as a click chemistry tool, incorporating an azide group that participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) and strain-promoted alkyne-azide cycloaddition (SPAAC) with alkyne, DBCO, or BCN-containing molecules, expanding its utility in biological research applications.
  13. Stable Isotope

    5-Ethynyl-2'-deoxyuridine-13C is a stable isotope-labeled analogue of 5-Ethynyl-2'-deoxyuridine (EdU), targeting cellular DNA during replication. This compound is incorporated into DNA and allows for visualization through a copper-catalyzed azide-alkyne cycloaddition (CuAAc) in Click chemistry applications. EdU-13C serves as a sensitive and efficient probe for assessing cell proliferation, making it invaluable for research in cell biology and drug development. Additionally, it can function as a linker in the synthesis of PROTACs, facilitating studies in targeted protein degradation.
  14. Stable Isotope

    NH2-C2-NH-Boc-d4 is a deuterium-labeled variant of the PROTAC linker NH2-C2-NH-Boc. This alkyl chain-based linker facilitates the development of proteolysis-targeting chimeras (PROTACs) by enhancing the stability and efficacy of the resultant compounds. Its incorporation in PROTAC synthesis enables precise investigation of protein degradation mechanisms and aids in the advancement of targeted protein modulation research.
  15. Stable Isotope

    5-Ethynyl-2'-deoxyuridine-13C2 is a stable isotope-labeled analogue of 5-Ethynyl-2'-deoxyuridine, specifically incorporating two carbon-13 atoms. This compound functions primarily in studying DNA replication, as it is incorporated into cellular DNA and subsequently detected through a fluorescent azide in a "Click" reaction. Key applications include cell proliferation assays and the synthesis of PROTACs, leveraging its alkyne functionality for copper-catalyzed azide-alkyne cycloaddition. Its use in research facilitates advanced studies in nucleic acid dynamics and targeted protein degradation.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. Stable Isotope

    Raloxifene-d4 is a deuterium-labeled derivative of Raloxifene, a selective estrogen receptor modulator (SERM) derived from benzothiophene. This compound exhibits estrogen-agonistic activity on bone and lipid metabolism while antagonizing estrogen effects in breast and uterine tissues. Raloxifene-d4 is valuable for research in breast cancer and osteoporosis, providing a stable isotope for traceable studies in endocrine signaling pathways.
  33. Stable Isotope

    Equilin-d4 is a deuterium-labeled derivative of Equilin (7-Dehydroestrone), a significant member of the estrogenic compounds family. It primarily serves as a stable isotope for tracing studies in biochemical research. Equilin has been shown to promote the growth of cortical neurons through an NMDA receptor-dependent mechanism, highlighting its potential as a valuable tool in neuroscience and hormonal studies.
  34. Stable Isotope

    (Rac)-Hexestrol-d4 is a deuterium-labeled analog of (Rac)-Hexestrol, serving as a stable isotope for research applications. This compound is utilized in metabolic studies and tracing experiments to provide insights into the metabolism and pharmacokinetics of estrogenic compounds. Its isotopic labeling aids in enhancing the sensitivity and accuracy of analytical techniques, making it an essential tool for scientists investigating steroid hormone dynamics.
  35. Stable Isotope

    Estradiol valerianate-d9 is a deuterium-labeled derivative of Estradiol valerianate, a synthetic estrogen. This compound serves as a stable isotope for use in pharmacokinetic studies, metabolic tracking, and other applications requiring precise quantification of endogenous estrogens. It is useful in research on hormone replacement therapies and estrogen receptor interactions, enabling detailed investigations into hormonal modulation in various biological systems.
  36. Stable Isotope

    Raloxifene-d4 hydrochloride is a deuterium-labeled derivative of Raloxifene, a selective estrogen receptor modulator (SERM) derived from benzothiophene. This compound exhibits estrogen-agonistic effects on bone and lipid metabolism, while demonstrating estrogen-antagonistic properties in breast and uterine tissues. Raloxifene-d4 hydrochloride is utilized in the investigation of breast cancer and osteoporosis, facilitating research into the nuances of estrogen signaling pathways and therapeutic development.
  37. Stable Isotope

    (Rac)-Hexestrol-d6 is a deuterium-labeled analog of (Rac)-Hexestrol, primarily utilized as a stable isotope in biochemical research. This compound serves as a valuable tracer in studies involving hormonal interactions and metabolic pathways. Its unique labeling allows for enhanced detection and quantification in various analytical techniques, making it an essential tool for researchers investigating estrogenic activity and receptor binding assays.
  38. Stable Isotope

    Diisopropyl phthalate-d4 is a deuterium-labeled derivative of Diisopropyl phthalate (DiPP), serving as a stable isotope for various scientific applications. This compound is a phthalate diester commonly utilized as a plasticizer in consumer products. It exhibits weak binding affinity to the recombinant human estrogen receptor, demonstrating an IC50 value of 41,000 μM, making it useful in studies related to endocrine disruption and environmental toxicology.
  39. Stable Isotope

    Diethylstilbestrol-d3 is a deuterium-labeled derivative of Diethylstilbestrol, a synthetic nonsteroidal estrogen. This stable isotope can be utilized in various biochemical and pharmaceutical research applications, including metabolic studies and the investigation of estrogen receptor interactions. Its use enhances the understanding of pharmacokinetics and dynamics of estrogenic compounds in biological systems.
  40. Stable Isotope

    Estradiol benzoate-d3 is a deuterium-labeled derivative of Estradiol benzoate, a proagent of the steroid sex hormone estradiol. This compound possesses mild anabolic and metabolic properties, influencing various physiological processes, including enhancing blood coagulability. It is primarily utilized in research applications focused on hormone activity, steroid metabolism, and the effects of estradiol in biological systems.
  41. Stable Isotope

    α-Zearalenol-d4 is a deuterated isotope of α-Zearalenol, a mycotoxin known for its strong affinity for estrogen receptors. As a derivative of zearalenone, it demonstrates significant xenoestrogenic properties that can lead to reproductive disorders in various animal models. This stable isotope is valuable for biochemical and pharmacological studies involving estrogen receptor signaling and mycotoxin metabolism.
  42. Stable Isotope

    Estradiol valerianate-d4 is a deuterium-labeled derivative of Estradiol valerianate, a synthetic estrogen. It plays a crucial role in hormone replacement therapy by providing a stable isotope for metabolic studies and tracer applications. The compound is essential in understanding estrogen metabolism and dynamics in biological systems.
  43. Stable Isotope

    Raloxifene 4'-glucuronide-d4 is a deuterated stable isotope of Raloxifene 4'-glucuronide, a primary metabolite of Raloxifene. This compound is primarily formed through the action of UGT1A10 and UGT1A8 enzymes. Raloxifene 4'-glucuronide exhibits binding to the estrogen receptor with an IC50 of 370 μM. It functions as a selective estrogen receptor modulator, activating the TGFβ3 promoter as a full agonist at nanomolar concentrations while also inhibiting expression from the estrogen response element-containing vitellogenin promoter. This makes it a valuable tool for studying estrogen receptor activity and metabolism in chemical research.
  44. Stable Isotope

    (Rac)-Zearalanone-d6 is a stable isotope of the mycotoxin Zearalanone, a nonsteroidal estrogenic compound produced by Fusarium species commonly found in various grains. This compound acts as an estrogen receptor agonist, demonstrating significant estrogenic and anabolic effects across multiple animal species, which can adversely impact the reproductive system. (Rac)-Zearalanone-d6 can be used for research applications involving environmental monitoring, toxicology studies, and investigations into estrogenic activity in biological systems.
  45. Stable Isotope

    Zeranol-d5 (mixture of diastereomers) is a deuterium-labeled derivative of Zeranol, acting as an estrogen receptor agonist. This compound is primarily utilized in research examining estrogenic activity and its effects on growth promotion in livestock. Its stable isotope nature allows for precise tracking in metabolic studies and contributes to understanding the role of mycoestrogens in environmental and health-related contexts.
  46. Stable Isotope

    Bazedoxifene-d4 is a deuterium-labeled analog of Bazedoxifene, a nonsteroidal selective estrogen receptor modulator (SERM) that exhibits a potent affinity for estrogen receptors ERα and ERβ, with IC50 values of 23 nM and 99 nM, respectively. This compound is utilized in research focused on osteoporosis and has been shown to inhibit IL-6/GP130 protein-protein interactions, making it relevant for studies related to pancreatic cancer. Its stable isotope labeling facilitates advanced metabolic and pharmacokinetic investigations.
  47. Stable Isotope

    Dienestrol-d2 is a deuterium-labeled derivative of Dienestrol, functioning as a stable isotope. This compound can be utilized in quantitative analytical techniques, such as liquid chromatography-mass spectrometry (LC-MS), to study the pharmacokinetics and metabolism of estrogens. Its unique isotopic labeling enhances sensitivity and specificity in biological research applications.
  48. Stable Isotope

    (Rac)-Hexestrol-d6-1 is a deuterium-labeled derivative of the synthetic non-steroidal estrogen, (Rac)-Hexestrol. It serves as a stable isotope for use in various biological and chemical research applications, including metabolic studies and pharmacokinetic investigations. This compound aids in understanding the behavior and mechanisms of estrogen-related processes in different biological systems.
  49. Stable Isotope

    17-Epiestriol-d5-1 is a deuterated form of 17-Epiestriol, a selective estrogen receptor (ER) β agonist. This compound functions as an effective inhibitor of vascular cell adhesion molecule VCAM-1 expression induced by tumor necrosis factor α (TNFα) and prevents the nuclear translocation of NF-κB. Additionally, 17-Epiestriol-d5-1 promotes the expression of endothelial nitric oxide synthase at both mRNA and protein levels. It serves as a valuable tool in research exploring estrogen receptor signaling and its implications in cardiovascular and inflammatory responses.
  50. Stable Isotope

    Bazedoxifene-d4 acetate is a deuterium-labeled form of Bazedoxifene, a nonsteroidal selective estrogen receptor modulator (SERM) that demonstrates potent activity against estrogen receptors ERα and ERβ with IC50 values of 23 nM and 99 nM, respectively. This stable isotope is valuable for research involving osteoporosis and also serves as an inhibitor of IL-6/GP130 protein-protein interactions, making it relevant for studies in pancreatic cancer.

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