Isotope-Labeled Compounds

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  1. Stable Isotope

    Cinacalcet-d4 hydrochloride is a deuterated form of Cinacalcet, an allosteric agonist of the calcium-sensing receptor (CaR). This stable isotope is employed in research to track and quantify metabolic processes involving the modulation of calcium homeostasis. It is particularly relevant in studies focused on cardiovascular diseases and related therapeutic interventions.
  2. Stable Isotope

    Telcagepant-d8 is a deuterium-labeled variant of Telcagepant, a potent orally active antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits binding affinities (Kis) of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Telcagepant-d8 is primarily utilized in pharmacokinetic studies and metabolic research, providing a valuable tool for investigating CGRP-related pathways and receptor interactions in various biological systems.
  3. Stable Isotope

    Tildacerfont-d8 is a deuterium-labeled derivative of Tildacerfont, a potent and orally bioavailable antagonist of the corticotropin-releasing factor type 1 (CRF1) receptor. It effectively lowers levels of adrenocorticotropic hormone (ACTH) and adrenal androgens, demonstrating a favorable safety profile. Tildacerfont-d8 is valuable for research into congenital adrenal hyperplasia and related hormonal regulation studies, facilitating the investigation of CRF1 receptor dynamics.
  4. Stable Isotope

    Nicotinamide N-oxide-d4 is a deuterium-labeled derivative of Nicotinamide N-oxide, which serves as a stable isotope for analytical studies. As a notable in vivo metabolite of nicotinamide, Nicotinamide N-oxide exhibits potent and selective antagonistic activity against the CXCR2 receptor. This compound is valuable for research applications involving receptor signaling, metabolic pathways, and the study of inflammatory responses.
  5. Stable Isotope

    Dopamine-d3 hydrochloride is a deuterium-labeled analog of dopamine, serving as a stable isotope for research applications. It is utilized in studies involving neurotransmitter dynamics and metabolic pathways, providing insights into dopamine-related physiological processes. This reagent is valuable in mass spectrometry and tracer studies, aiding in the exploration of neurological disorders and drug interactions.
  6. Stable Isotope

    L-DOPA-2,5,6-d3 is a deuterium-labeled form of L-DOPA, a metabolic precursor to the neurotransmitter dopamine. This stable isotope enables researchers to study dopamine synthesis and metabolism in vivo, particularly its ability to cross the blood-brain barrier and its subsequent conversion to dopamine in neural tissues. L-DOPA-2,5,6-d3 is instrumental in neurochemical studies, including investigations of neurological disorders and the evaluation of therapeutic strategies targeting dopaminergic signaling.
  7. Stable Isotope

    L-DOPA-13C is a stable isotope-labeled form of L-DOPA, which serves as a metabolic precursor to the neurotransmitter dopamine. It effectively crosses the blood-brain barrier and is converted to dopamine in the central nervous system. L-DOPA-13C is utilized in research for understanding neurotransmitter dynamics and exploring its role in Parkinson's disease and related neurological conditions. Additionally, it exhibits anti-allodynic properties, making it relevant for studies on pain modulation.
  8. Stable Isotope

    L-DOPA-d6 is a deuterium-labeled form of L-DOPA, a critical precursor in the biosynthesis of the neurotransmitter dopamine. This stable isotope enables precise tracing and quantification in metabolic studies involving neurotransmitter dynamics, particularly in the context of neurological disorders. L-DOPA-d6 is utilized in research applications focused on dopamine-related pathways, including the investigation of Parkinson's disease and its associated therapeutic strategies.
  9. Stable Isotope

    L-DOPA-13C6 is a stable isotope-labeled form of L-DOPA, a critical metabolic precursor for the synthesis of the neurotransmitter dopamine. This compound effectively crosses the blood-brain barrier and is metabolized into dopamine within the central nervous system, making it a key agent in research related to neurotransmitter pathways. L-DOPA-13C6 is particularly valuable in studies investigating the pharmacokinetics of dopamine replacement therapies and has implications for understanding and treating Parkinson's disease.
  10. Stable Isotope

    Amisulpride-d5 is a deuterium-labeled derivative of Amisulpride, a selective antagonist of the dopamine D2 and D3 receptors. It exhibits high affinity with Kis of 2.8 nM and 3.2 nM for human D2 and D3 receptors, respectively. This stable isotope is utilized in pharmacokinetic studies, metabolic research, and tracer studies to investigate the pharmacological properties and dynamics of dopamine receptor interactions.
  11. Stable Isotope

    Emtricitabine-13C,15N2 is a stable isotope-labeled version of Emtricitabine, a nucleoside reverse transcriptase inhibitor (NRTI). With an EC50 of 0.01 μM in peripheral blood mononuclear cells (PBMCs), it exhibits potent antiviral activity against HIV. This labeled compound is primarily used in pharmacokinetic studies and metabolic research, aiding in understanding drug efficacy and dynamics within biological systems.
  12. Stable Isotope

    Oltipraz-d3 is a deuterium-labeled derivative of Oltipraz, primarily targeting hypoxia-inducible factor 1-alpha (HIF-1α). It demonstrates inhibitory effects on HIF-1α activation in a time-dependent manner, fully suppressing its induction at concentrations of 10 μM or greater, with an IC50 value of 10 μM. Additionally, Oltipraz acts as a potent activator of Nrf2, making it a valuable reagent for studies investigating cellular responses to hypoxic conditions and oxidative stress.
  13. Stable Isotope

    Lopinavir-d7 is a deuterated derivative of Lopinavir, a selective peptidomimetic inhibitor targeting the HIV-1 protease. It demonstrates potent activity, with Ki values ranging from 1.3 to 3.6 pM against both wild-type and mutant HIV proteases, effectively preventing HIV-1 maturation and subsequent infectivity. Additionally, Lopinavir has been identified as an inhibitor of SARS-CoV 3CLpro, showcasing an IC50 of 14.2 μM, making it valuable for research in virology and antiviral drug development.
  14. Stable Isotope

    Atazanavir-d6 is a deuterium-labeled form of Atazanavir, a selective inhibitor of HIV-1 protease. Recognized for its capability as a CYP3A4 substrate and inhibitor, it also exerts dual effects as both an inhibitor and inducer of P-glycoprotein (P-gp). In addition, Atazanavir demonstrates antiviral activity by inhibiting the SARS-CoV 3CLpro with an IC50 of 3.49 μM, making it a valuable tool for research in HIV and coronavirus-related studies.
  15. Stable Isotope

    Raltegravir-d6 is a deuterated derivative of Raltegravir, a well-established integrase (IN) inhibitor employed in the management of HIV infection. This stable isotope-labeled compound is instrumental for use in pharmacokinetic studies, enabling precise tracking of drug metabolism and distribution in biological systems. Its application in research contributes to a better understanding of drug dynamics and efficacy in antiretroviral therapy.
  16. Stable Isotope

    Atazanavir-d15 is a stable isotope-labeled form of Atazanavir, an effective selective inhibitor of HIV-1 protease. This compound is utilized in biochemical research to help elucidate drug metabolism and pharmacokinetics. Its unique labeling allows for precise tracking in biological systems, enhancing studies focused on HIV infection and treatment strategies.
  17. Stable Isotope

    (rel)-Lopinavir-d8 is a deuterium-labeled derivative of Lopinavir, a selective peptidomimetic inhibitor targeting HIV-1 protease. This compound demonstrates high potency, with inhibition constants ranging from 1.3 to 3.6 pM against both wild-type and mutant forms of the enzyme, effectively hindering HIV maturation and infectivity. Additionally, (rel)-Lopinavir-d8 exhibits activity as an inhibitor of the SARS-CoV 3CLpro with an IC50 of 14.2 μM, making it a valuable tool for HIV and coronavirus research applications.
  18. Stable Isotope

    Elvitegravir-d5 is a deuterated form of Elvitegravir, a potent integrase inhibitor targeting HIV-1 and HIV-2 strains. It demonstrates impressive inhibitory activity with IC50 values of 0.7 nM, 2.8 nM, and 1.4 nM against HIV-1IIIB, HIV-2EHO, and HIV-2ROD, respectively. This stable isotope is valuable for biochemical and pharmacokinetic studies, offering insights into HIV integrase function and drug metabolism in research applications.
  19. Stable Isotope

    Glurate-d5, a deuterium-labeled derivative of Glurate, primarily functions as an acylating agent. It is utilized in the development of antiviral compounds, particularly those effective against retroviruses, including herpes virus and HIV. Additionally, Glurate-d5 plays a crucial role in the synthesis of acyclic nucleoside derivatives and 5-hydroxyhexanoic acid, making it valuable for various biochemical research applications.
  20. Stable Isotope

    Amprenavir-d4-1 is a deuterated form of Amprenavir, an effective HIV protease inhibitor with a Ki value of 0.6 nM. In addition to its antiviral activity, Amprenavir also demonstrates inhibition of the SARS-CoV 3CL pro enzyme with an IC50 of 1.09 μM. This stable isotope is valuable for research applications, including pharmacokinetics and metabolic studies of related compounds in virology and drug development contexts.
  21. Stable Isotope

    Atazanavir-d18 is a stable isotope-labeled version of Atazanavir, a selective inhibitor of the HIV-1 protease. This compound is utilized in biochemical and pharmacokinetic studies, providing valuable insights into the metabolism and distribution of Atazanavir in biological systems. Its stable isotope labeling allows for precise quantification and tracking in research applications related to HIV treatment and drug development.
  22. Stable Isotope

    Ditiocarb-d10 sodium is a deuterated form of sodium diethyldithiocarbamate, functioning as a stable isotope label. This compound acts primarily as a copper chelator and exhibits significant antioxidant properties, anti-tumor effects, immunomodulatory activity, and potential anti-HIV functions. Ditiocarb-d10 sodium is useful in research concerning tumor biology, inflammatory responses, and immune system modulation.
  23. Stable Isotope

    Maraviroc-d6 is a deuterium-labeled analog of Maraviroc, a selective antagonist of the CCR5 receptor. This compound is primarily utilized in research to study HIV infection and the mechanisms of CCR5-mediated viral entry. Its stable isotope labeling allows for improved tracking and analysis in biological assays, facilitating investigations into antiviral drug development and efficacy.
  24. Stable Isotope

    Etravirine-13C3 is a stable isotope-labeled derivative of Etravirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI) utilized in HIV treatment. This compound serves as a valuable tool for metabolic studies and pharmacokinetic analyses involving Etravirine, aiding in the understanding of its biochemical properties and interactions. Its isotopic labeling facilitates precise measurements in various research applications related to HIV dynamics and drug metabolism.
  25. Stable Isotope

    Rilpivirine-d6 hydrochloride is a deuterium-labeled analog of Rilpivirine, targeting the HIV-1 reverse transcriptase enzyme. This stable isotope variant enables precise quantification and tracking of Rilpivirine in pharmacokinetic studies and metabolic research. Its application is crucial for understanding drug metabolism and enhancing the development of antiretroviral therapies.
  26. Stable Isotope

    Dolutegravir-d5 is a deuterium-labeled analog of Dolutegravir, a potent inhibitor of HIV-1 integrase strand transfer. It demonstrates exceptional antiviral activity with an IC50 value of 2.7 nM against HIV-1 integrase and an IC50 of 0.51 nM for suppressing viral replication in peripheral blood mononuclear cells. Additionally, Dolutegravir maintains strong efficacy against key HIV-1 variants, including Y143R, N155H, and G140S/Q148H mutants, with EC50 values ranging from 3.6 to 5.8 nM. This stable isotope is valuable for pharmacokinetic studies and metabolic research in HIV treatment.
  27. Stable Isotope

    Emtricitabine-15N,d2 is a stable isotope-labeled form of Emtricitabine, a nucleoside reverse transcriptase inhibitor (NRTI). This compound exhibits antiviral activity against HIV with an EC50 of 0.01 μM in PBMC cells. Emtricitabine-15N,d2 is valuable for studies involving pharmacokinetics and drug metabolism, enabling precise tracking of the compound in biological systems.
  28. Stable Isotope

    Lopinavir-d8 is a deuterated form of the potent HIV-1 protease inhibitor Lopinavir, functioning primarily by inhibiting the enzyme's activity, which is crucial for viral maturation. With an affinity (Kis) ranging from 1.3 to 3.6 pM against both wild-type and mutant strains of HIV protease, Lopinavir-d8 effectively blocks HIV-1 infectivity. Additionally, it serves as an inhibitor of SARS-CoV 3CLpro, exhibiting an IC50 value of 14.2 μM, making it valuable for research on viral proteases and potential therapeutic applications in retroviral and coronavirus research.
  29. Stable Isotope

    Ditiocarb-d10 (Deuterium-labeled Diethyldithiocarbamic acid) serves as a stable isotope for research applications. Primarily, it acts as an accelerator in copper cementation processes. Additionally, Ditiocarb has been shown to reduce the incidence of HIV infections and may enhance adjuvant immunotherapy strategies in high-risk breast cancer research. This stable isotope variant enables more precise tracking and analysis in related biochemical and clinical studies.
  30. Stable Isotope

    ZK-316 is a stable isotope and a potent broad-spectrum non-nucleoside reverse transcriptase inhibitor (NNRTI) that demonstrates EC50 values ranging from 0.99 to 75.1 nM. This compound is essential for HIV research, facilitating the understanding of viral replication and the development of antiretroviral therapies. Its efficacy makes it a valuable tool for studying the mechanisms of HIV infection and resistance to treatment.
  31. Stable Isotope

    Nevirapine-d3 is a deuterated form of Nevirapine, a non-nucleoside inhibitor targeting HIV-1 reverse transcriptase, with a Ki of 270 μM. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research involving HIV/AIDS treatments. Its incorporation into studies can enhance the understanding of drug pharmacodynamics and metabolic pathways in the context of antiviral therapies.
  32. Stable Isotope

    Bictegravir-d7 is a deuterium-labeled form of Bictegravir, a potent inhibitor of HIV-1 integrase. It exhibits an IC50 of 7.5 nM, demonstrating strong inhibitory activity against the virus. This stable isotope is primarily utilized in research applications that require precise tracking of compound metabolism and pharmacokinetics in biological systems.
  33. Stable Isotope

    Nevirapine-d8 is a deuterated derivative of Nevirapine, serving as a stable isotope. Nevirapine functions as a non-nucleoside inhibitor of HIV-1 reverse transcriptase, demonstrating a Ki value of 270 μM. This reagent is valuable for pharmacokinetic studies and the development of analytical methods in HIV research. Its stable isotope labeling enables precise quantification and tracing in various biological assays.
  34. Stable Isotope

    Etravirine-d8 is a deuterium-labeled variant of Etravirine, a non-nucleoside reverse transcriptase inhibitor (NNRTI) targeting the HIV reverse transcriptase enzyme. This stable isotope is utilized in research to track pharmacokinetics and metabolic pathways of Etravirine, enhancing the understanding of its biological activity in HIV treatment. Etravirine-d8 serves as a valuable tool in drug development and pharmacological studies.
  35. Stable Isotope

    Finafloxacin-d4 hydrochloride is a deuterium-labeled derivative of Finafloxacin, serving as a stable isotope. This compound can be utilized in pharmacokinetic studies and metabolic research to track drug metabolism and distribution in biological systems. Its labeled form allows for enhanced detection and quantification in analytical techniques, supporting research applications in drug development and therapeutic monitoring.
  36. Stable Isotope

    Trofosfamide-d4 is a stable isotope-labeled form of Trofosfamide, an orally bioavailable oxazaphosphorine derivative known for its antineoplastic properties. The deuterium labeling allows for enhanced tracking and quantification in metabolic studies. This reagent is suitable for research applications such as pharmacokinetics, drug metabolism, and isotope labeling studies in oncology research.
  37. Stable Isotope

    Cletoquine-d4 is a deuterium-labeled derivative of Cletoquine, the primary active metabolite of Hydroxychloroquine. This stable isotope is utilized in pharmacokinetic studies and metabolic pathway investigations due to its unique labeling. Cletoquine exhibits notable antimalarial activity and has demonstrated efficacy against the chikungunya virus (CHIKV), alongside potential therapeutic implications for autoimmune diseases. Its use in research can enhance the understanding of drug metabolism and therapeutic mechanisms.
  38. Stable Isotope

    Cletoquine-d4-1 is a deuterium-labeled derivative of Cletoquine, a significant active metabolite of Hydroxychloroquine. This compound is produced by the liver through the action of CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine-d4-1 exhibits antiviral activity against the chikungunya virus (CHIKV) and possesses antimalarial properties, making it valuable in research applications focused on malaria and autoimmune disease therapies.
  39. Stable Isotope

    Cletoquine-d4 Oxalate is a stable isotope of Cletoquine, a significant active metabolite of Hydroxychloroquine. This compound, produced in the liver by various cytochrome P450 isoenzymes, exhibits antimalarial properties and shows promise in the treatment of autoimmune diseases. Additionally, as a Chloroquine derivative, Cletoquine-d4 Oxalate has demonstrated antiviral activity against the chikungunya virus (CHIKV), making it a valuable reagent for research applications in virology and pharmacology.
  40. Stable Isotope

    Umifenovir-d6 hydrochloride is a deuterated form of Umifenovir hydrochloride, a broad-spectrum antiviral agent. This compound demonstrates potent activity against both enveloped and non-enveloped viruses, primarily functioning by inhibiting the fusion of viral particles with host cells. Umifenovir hydrochloride is notably effective against influenza viruses and has shown significant in vitro inhibition of SARS-CoV-2. Additionally, it exhibits anti-inflammatory properties, making it a valuable tool for research in virology and therapeutic approaches targeting viral infections.
  41. Stable Isotope

    Valganciclovir-d8 is a deuterium-labeled derivative of Valganciclovir, which serves as a prodrug for ganciclovir. This stable isotope-labeled compound is widely utilized in pharmacokinetic studies and metabolic research to trace drug metabolism and bioavailability, enabling a detailed understanding of its pharmacological effects. Its applications extend to studies on viral infections and potential therapeutic outcomes in disease contexts such as cytomegalovirus retinitis.
  42. Stable Isotope

    Valganciclovir-d5 TFA is a deuterium-labeled derivative of valganciclovir, functioning as a stable isotope. As a prodrug of ganciclovir, it exhibits antiviral activity primarily against cytomegalovirus (CMV) infections. This reagent is valuable for metabolic studies, pharmacokinetic analyses, and tracing the pharmacodynamics of antiviral therapies in research applications.
  43. Stable Isotope

    Brincidofovir-d6 is a deuterated form of Brincidofovir, functioning as a stable isotope for research applications. As a lipid-conjugated prodrug of Cidofovir, this compound exhibits potent antiviral activity against a wide range of DNA viruses, including cytomegalovirus, adenovirus, and orthopoxviruses. It is particularly valuable in studies focused on viral pathogenesis, therapeutic efficacy, and pharmacokinetics of antiviral agents. The isotopic labeling of Brincidofovir enhances the ability to track and quantify the compound's behavior in biological systems.
  44. Stable Isotope

    Naringenin-d4 is a deuterated derivative of Naringenin, functioning as a stable isotope. Its primary biological activities include potent anti-inflammatory and antioxidant effects. Naringenin-d4 serves as a valuable tool for research applications, particularly in studies focused on inflammation, oxidative stress, and viral infections, including anti-dengue virus (DENV) investigations.
  45. Stable Isotope

    Quinine-d3 is a deuterium-labeled derivative of quinine, primarily used as a stable isotope in chemical research. Quinine is an alkaloid isolated from the cinchona tree, known for its efficacy as an antimalarial agent and its role as a potassium channel inhibitor. It specifically inhibits wild-type mouse Slo3 (KCa5.1) channel currents induced by voltage pulses, exhibiting an IC50 of 169 μM. This reagent facilitates studies in pharmacology and biochemistry, enabling precise tracking and quantification in various applications.
  46. Stable Isotope

    Fluticasone propionate-d5 is a deuterium-labeled derivative of fluticasone propionate, a potent topical anti-inflammatory corticosteroid. This compound selectively binds to the glucocorticoid receptor, exhibiting an absolute affinity (KD) of 0.5 nM, and demonstrates minimal interaction with other steroid receptors. It is primarily utilized in research involving anti-inflammatory and potential antiviral activities, making it a valuable reagent for studies focused on corticosteroid receptor mechanism and function.
  47. Stable Isotope

    Vapendavir-d5 is a deuterium-labeled derivative of Vapendavir, a potent enteroviral capsid binder. This stable isotope is utilized in research to study the mechanisms of action against enterovirus 71 (EV71), exhibiting significant antiviral activity with EC50 values ranging from 0.5 to 1.4 μM across various EV71 strains. Vapendavir-d5 serves as a valuable tool in understanding enteroviral infections and developing therapeutic strategies.
  48. Stable Isotope

    Pleconaril-d4 is a deuterated analog of Pleconaril, designed as a stable isotope for advanced chemical research. This labeled compound serves as a valuable tool for tracing and quantifying Pleconaril-related metabolic pathways and interactions. Its use in studies involving viral infections, particularly enteroviruses, enhances understanding of drug efficacy and pharmacokinetics in biological systems.
  49. Stable Isotope

    Fmoc-leucine-15N is a stable isotope-labeled derivative of leucine, featuring a nitrogen-15 isotope, which facilitates studies in metabolic tracing and protein labeling. This compound is widely utilized in peptide synthesis and NMR spectroscopy, enabling researchers to gain insights into protein structure and dynamics. Its incorporation into peptides allows for enhanced monitoring of metabolic pathways and interactions in biological systems.
  50. Stable Isotope

    Pirlindole-d4 is a deuterium-labeled analogue of Pirlindole, serving as a stable isotope for research applications. This compound is primarily utilized in metabolic studies and tracer experiments due to its isotopic labeling, facilitating the investigation of pharmacokinetics and drug metabolism. Pirlindole itself is known for its role as a serotonin and norepinephrine reuptake inhibitor, contributing to its therapeutic potential in the treatment of depression and other mood disorders.

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