Isotope-Labeled Compounds

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  1. Stable Isotope

    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.
  2. Stable Isotope

    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.
  3. Stable Isotope

    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.
  4. Stable Isotope

    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.
  5. Stable Isotope

    (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.
  6. Stable Isotope

    (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.
  7. Stable Isotope

    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.
  8. Stable Isotope

    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.
  9. Stable Isotope

    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.
  10. Isotope-Labeled Compounds

    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.
  11. Stable Isotope

    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.
  12. Stable Isotope

    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.
  13. Stable Isotope

    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.
  14. Stable Isotope

    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.
  15. Stable Isotope

    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.
  16. Stable Isotope

    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.
  17. Stable Isotope

    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.
  18. Stable Isotope

    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.
  19. Stable Isotope

    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.
  20. Stable Isotope

    Anthracene-9-carboxylic acid-d9 is a deuterium-labeled derivative of anthracene-9-carboxylic acid. This compound primarily functions as a stable isotope and is widely utilized in research to study calcium-activated chloride currents (CaCCs) across various cell types, including smooth muscle, epithelial, and salivary gland cells. Its deuterium labeling enhances analytical sensitivity in experiments, facilitating more accurate investigations into cellular signaling and ion channel activity.
  21. Stable Isotope

    Niflumic Acid-d5 is a deuterium-labeled derivative of Niflumic acid, which acts primarily as a calcium-activated chloride channel blocker. This compound exhibits significant analgesic and anti-inflammatory properties, making it useful in the management of conditions such as rheumatoid arthritis. Its stable isotope form is valuable for research applications in pharmacokinetics, metabolic studies, and mechanistic investigations of calcium channel modulation.
  22. Stable Isotope

    γ-Aminobutyric acid-d6 is a deuterium-labeled form of γ-Aminobutyric acid, a crucial inhibitory neurotransmitter in the mammalian central nervous system. This compound primarily targets ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), playing a significant role in regulating neuronal excitability. It is useful in research applications focused on neurotransmitter dynamics, GABAergic signaling, and metabolic studies involving stable isotopes.
  23. Stable Isotope

    γ-Aminobutyric acid-d2 is a deuterium-labeled form of γ-Aminobutyric acid, a critical inhibitory neurotransmitter in the mammalian central nervous system. It functions by binding to both ionotropic GABA receptors (GABAA) and metabotropic GABA receptors (GABAB), playing a vital role in neuronal signaling and modulation. This stable isotope is particularly useful in research applications involving metabolic tracing, pharmacokinetics, and the study of neurochemical pathways.
  24. Stable Isotope

    Methionine-d3 is a deuterium-labeled form of Methionine, serving as a stable isotope useful in metabolic studies. This compound is known for its chemoprotective properties and its ability to inhibit neuronal activity via GABAA receptor activation. Methionine-d3 is valuable for researchers conducting studies in neurobiology and metabolic pathways, offering insights into the roles of methionine in cellular processes.
  25. Stable Isotope

    p-Hydroxybenzaldehyde-d4 is a deuterium-labeled variant of p-Hydroxybenzaldehyde. It primarily serves as a stable isotope for advanced analytical applications. This compound is known for its presence in Dendrocalamus asper bamboo shoots and exhibits antagonistic activity on the GABAA receptor α1β2γ2S subtype at elevated concentrations. It is useful in various research applications, including metabolic studies and receptor pharmacology.
  26. Stable Isotope

    Propofol-d18 is a deuterium-labeled derivative of Propofol, primarily utilized as a stable isotope in research. This compound effectively activates GABAA receptors, leading to enhanced inhibitory neurotransmission while simultaneously inhibiting excitatory synaptic transmission mediated by glutamate receptors. Propofol-d18 is valuable for studies investigating the neuropharmacology of anesthetics and the dynamics of synaptic transmission.
  27. Stable Isotope

    Tetrahydrodeoxycorticosterone-d3 is a deuterated form of Tetrahydrodeoxycorticosterone, a potent positive allosteric modulator of the GABAA receptor. This neurosteroid exhibits significant neuroinhibitory properties, making it a valuable tool in neuroscience research. Its stable isotope labeling allows for precise tracking and quantification in various biological assays and studies related to neuropharmacology and neurobiology.
  28. Stable Isotope

    Furosemide-d5 is a deuterium-labeled derivative of furosemide, primarily targeting the Na+/K+/2Cl- cotransporters, NKCC1 and NKCC2. This compound acts as a potent loop diuretic, exhibiting significant biological activity in the management of conditions such as congestive heart failure, hypertension, and edema. Additionally, furosemide-d5 can function as a GABAA receptor antagonist, demonstrating enhanced selectivity for α6-containing receptors. It serves as a valuable tool for biochemical research and pharmacokinetic studies involving furosemide.
  29. Stable Isotope

    17β-Estradiol sulfate-d4 sodium is a deuterium-labeled derivative of 17β-Estradiol sulfate, commonly referred to as β-Estradiol 3-sulfate sodium salt. This stable isotope is utilized in biochemical research to investigate the metabolism and pharmacokinetics of estrogenic compounds. Its applications extend to studies in neurobiology, endocrinology, and reproductive health, providing valuable insights into the hormonal modulation of various biological processes.
  30. Stable Isotope

    Riluzole-13C,15N2 is a stable isotope-labeled form of Riluzole, specifically incorporating 13C and 15N isotopes. Riluzole functions primarily as an anticonvulsant and is known to act as a use-dependent Na+ channel blocker. Additionally, it inhibits GABA uptake with an IC50 of 43 μM. This reagent is useful for tracer studies in metabolic research, pharmacokinetics, and drug mechanism investigations.
  31. Stable Isotope

    Propofol-d17 is a deuterium-labeled analog of Propofol, serving as a stable isotope for research applications. This compound acts primarily as a potent GABAA receptor agonist, effectively enhancing inhibitory synaptic transmission while simultaneously inhibiting glutamate receptor-mediated excitatory responses. Due to its significant antinociceptive properties, Propofol-d17 is valuable in studies focusing on pain modulation and anesthetic mechanisms.
  32. Stable Isotope

    Etiocholanolone-d5 is a deuterated form of Etiocholanolone, a metabolic product of testosterone. This compound serves as a neurosteroid with known positive allosteric modulation of the GABAA receptor, although it exhibits less potency compared to its enantiomer. Its unique isotopic labeling makes it valuable for tracing and quantification studies in metabolic research and pharmacokinetics, particularly in investigations related to anticonvulsant activity.
  33. Stable Isotope

    Acamprosate-d3 calcium is a deuterium-labeled form of Acamprosate calcium, a compound that acts as a GABA receptor agonist and modulates glutamatergic systems. This stable isotope is utilized in research to study the pharmacokinetics and dynamics of Acamprosate in various biological systems. Its unique labeling allows for precise tracking and analysis in metabolic studies and drug interaction investigations.
  34. Stable Isotope

    Baclofen-d4 is a deuterium-labeled variant of Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA). It acts as a selective agonist for metabotropic GABAB receptors, mimicking GABA's function to induce slow presynaptic inhibition. With its ability to effectively cross the blood-brain barrier, Baclofen-d4 is particularly valuable for research on muscle spasticity and related neurological conditions, providing insights into GABAB receptor dynamics and therapeutic applications.
  35. Stable Isotope

    Acamprosate-d6 calcium is a stable isotope-labeled form of Acamprosate calcium, functioning primarily as a GABA receptor agonist and modulating glutamatergic neurotransmission. This compound is crucial for research into alcohol dependence and withdrawal, as it helps investigate the biochemical pathways involved in these processes. The stable isotope labeling enhances the sensitivity and accuracy of analytical techniques, making it valuable for various pharmacological studies.
  36. Stable Isotope

    Alpidem-d14 is a stable isotope-labeled variant of Alpidem, a potent GABAA receptor ligand targeting the α1β2γ2 subunit with an IC50 of 17 nM. This compound is primarily investigated for its anxiolytic properties and influences various biological processes, including modulation of mitochondrial permeability and glutathione levels, leading to hepatocyte necrosis. Additionally, Alpidem-d14 is utilized in research focused on anxiety disorders, convulsive conditions, and the behavioral effects in stressed rodent models.
  37. Stable Isotope

    Baclofen-d5 hydrochloride is a deuterated analog of Baclofen, functioning as a selective agonist for the metabotropic GABAB receptor (GABABR). This compound closely mimics the action of γ-aminobutyric acid (GABA), facilitating slow presynaptic inhibition via GABAB signaling pathways. With its significant ability to penetrate the blood-brain barrier, Baclofen-d5 hydrochloride is valuable in studying muscle spasticity and related neurological conditions. Its stable isotope labeling further enhances its applications in metabolic and pharmacokinetic research.
  38. Stable Isotope

    Cipepofol-d6 is a deuterium-labeled derivative of Cipepofol, which acts as a gamma-aminobutyric acid (GABA) receptor potentiator. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Cipepofol. Its biological activity as a psychomotor stabilizing agent makes it valuable for studies related to anesthetic effects and neuropharmacology.
  39. Stable Isotope

    p-Hydroxybenzaldehyde-d5 is a stable isotope-labeled derivative of p-Hydroxybenzaldehyde. This compound, primarily recognized for its role as a major component in vanilla aroma, exhibits antagonistic effects on the GABAA receptor, specifically the α1β2γ2S subtype, at elevated concentrations. It is widely utilized in chemical research for studies involving receptor activity and metabolic tracking.
  40. Stable Isotope

    Etbicyphat-13C3 is a stable isotope-labeled variant of Etbicyphat, a potent competitive antagonist of GABA(A) receptors. This compound has been shown to induce epileptiform activities in hippocampal CA1 neurons and effectively binds to GABA(A)-benzodiazepine receptors. Its isotopic labeling facilitates detailed studies of receptor interactions and the dynamics of GABAergic neurotransmission in various research applications.
  41. Stable Isotope

    Propofol-d14 is a deuterium-labeled form of Propofol (2,6-Diisopropylphenol-d14) designed for stable isotope applications. It acts as a potent and direct agonist of the GABAA receptor, inhibiting excitatory synaptic transmission mediated by glutamate receptors. This compound exhibits antinociceptive properties and is primarily utilized in research related to sedation and hypnotic mechanisms.
  42. Stable Isotope

    γ-Aminobutyric acid-4,4-d2 is a deuterated form of γ-aminobutyric acid (GABA), a principal inhibitory neurotransmitter in the mammalian brain. This compound selectively binds to ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), modulating synaptic transmission and neuronal excitability. The stable isotope labeling allows for advanced metabolic studies and tracing applications in neuropharmacology and neuroscience research.
  43. Stable Isotope

    Isonipecotic acid-d9 is a deuterium-labeled analogue of Isonipecotic acid, which functions as a partial agonist at GABAA receptors. This stable isotope is valuable for pharmacokinetic studies and in vivo experimentation, providing insights into the metabolism and dynamics of GABAergic compounds. Researchers can employ Isonipecotic acid-d9 to explore mechanisms of action related to neurological disorders and the role of GABAA receptor modulation in various physiological processes.
  44. Stable Isotope

    3α,21-Dihydroxy-5α-pregnan-20-one-d3 is a deuterium-labeled derivative of the neurosteroid 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), which acts as a positive modulator of GABAA receptors. This compound enhances the response of neurons to low concentrations of GABA, specifically at the α4β1δ subtype of GABAA receptors in vitro. It serves as a valuable stable isotope labeled reagent for research focusing on neurosteroid activity and GABAergic modulation.
  45. Stable Isotope

    P-Hydroxybenzaldehyde-13C6 is a stable isotope-labeled derivative of p-Hydroxybenzaldehyde. This compound serves as a key component in vanilla flavor profiles and exhibits antagonistic activity on the α1β2γ2S subtype of the GABAA receptor at elevated concentrations. It is useful in various research applications, particularly in studies involving flavor chemistry and neuropharmacology.
  46. Stable Isotope

    Cipepofol-d6-2 is a deuterium-labeled derivative of Cipepofol, a gamma-aminobutyric acid (GABA) receptor potentiator and psychomotor stabilizing agent. This stable isotope compound is essential for studies involving pharmacokinetics and metabolic pathways of Cipepofol, facilitating precise tracking and analysis in research applications. It provides a valuable tool for investigating the effects and mechanisms of GABA modulation in nervous system functioning.
  47. Stable Isotope

    Etiocholanolone-d2 is a deuterium-labeled derivative of Etiocholanolone (5β-Androsterone), which serves as a stable isotope for research applications. As a metabolite of testosterone, Etiocholanolone exhibits anticonvulsant properties and acts as a positive allosteric modulator of the GABAA receptor, albeit with lower potency compared to its enantiomer. This reagent is essential for studies focused on neurosteroids and their mechanisms in the central nervous system.
  48. Stable Isotope

    Rac-Vigabatrin-13C,d2 is a stable isotope-labeled derivative of Vigabatrin, a potent and irreversible inhibitor of GABA transaminase. By inhibiting the catabolism of GABA, it increases the levels of this inhibitory neurotransmitter in the brain, making it an effective antiepileptic agent. This compound is valuable for research applications that require stable isotope labeling, such as metabolic studies and drug mechanism investigations.
  49. Stable Isotope

    4-Hydroxy midazolam methanoate-d5 is a deuterated derivative of 4-hydroxymidazolam, a significant metabolite of the benzodiazepine midazolam, which exhibits potent anxiolytic effects. This stable isotope is primarily utilized in pharmacokinetic studies and drug metabolism research, enabling precise tracking of midazolam metabolism and its active metabolites in biological systems. Its incorporation in analytical assays aids in understanding the pharmacodynamics and pharmacokinetics of benzodiazepines, facilitating advancements in therapeutic interventions.
  50. Stable Isotope

    Baclofen-d4-1 is a deuterium-labeled derivative of Baclofen, an orally active selective agonist of metabotropic GABAB receptors. By mimicking GABA's actions, Baclofen induces slow presynaptic inhibition, contributing to its activity in the central nervous system. This compound is particularly relevant for research on muscle spasticity and neurological disorders, facilitating studies involving pharmacokinetics and metabolic pathways.

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