Isotope-Labeled Compounds

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  1. Stable Isotope

    Iloprost-d4 is a deuterium-labeled analog of Iloprost, a synthetic derivative of prostacyclin (PGI2) that primarily targets the prostacyclin receptor (IP). This stable isotope is utilized in various biochemical research applications, including pharmacokinetic studies and metabolic profiling. Its unique isotopic labeling facilitates advanced analytical techniques and enhances the understanding of prostacyclin's role in vascular biology and therapeutic interventions.
  2. Stable Isotope

    Prostaglandin E1-d9 is a deuterium-labeled derivative of Prostaglandin E1, functioning as a potent ligand for prostanoid receptors. It exhibits high affinity with inhibitory constants of 1.1 nM, 2.1 nM, 10 nM, 33 nM, and 36 nM for mouse EP3, EP4, EP2, IP, and EP1 receptors, respectively. As a stable isotope, Prostaglandin E1-d9 is valuable in metabolic studies and pharmacokinetic research, facilitating the investigation of prostanoid signaling pathways and their physiological effects, including vasodilation.
  3. Stable Isotope

    Selexipag-d6 is a deuterium-labeled derivative of Selexipag, a potent and orally bioavailable agonist of the prostacyclin (PGI2) receptor. This stable isotope-labeled compound serves as a valuable tool in pharmacokinetic and metabolic studies, enabling researchers to trace metabolic pathways and evaluate the pharmacodynamics of prostacyclin receptor modulation. Selexipag-d6 is particularly useful in elucidating the pharmacological profiles and therapeutic potentials of compounds targeting PGI2 receptors in cardiovascular research.
  4. Stable Isotope

    trans-Isoferulic acid-d3 is a deuterium-labeled derivative of trans-Isoferulic acid, a naturally occurring aromatic acid derived from Clematis florida var. plena. This compound possesses notable anti-inflammatory properties, primarily through its ability to suppress nitric oxide (NO) and prostaglandin E2 (PGE2) production. Its mechanism of action involves the induction of Nrf2-dependent heme oxygenase-1 (HO-1), making it valuable for research into cellular stress responses and inflammation pathways.
  5. Isotope-Labeled Compound

    Misoprostol acid-d5 is a deuterium-labeled analog of Misoprostol acid, the active metabolite of Misoprostol. This compound is a synthetic analog of prostaglandin E1 (PGE1) and is rapidly absorbed, undergoing de-esterification in the gastrointestinal tract post oral administration. Misoprostol acid-d5 is instrumental in studying NSAID-induced gastric ulcers and is utilized in research related to labor induction. This isotope-labeled compound facilitates the investigation of metabolic pathways and pharmacokinetics in various biological systems.
  6. Stable Isotope

    MRE-269-d6 is a deuterium-labeled derivative of MRE-269, which is a selective agonist of the IP receptor and an active metabolite of selexipag. This stable isotope is valuable for metabolic studies, pharmacokinetic research, and tracer studies in vivo due to its unique mass properties. MRE-269-d6 facilitates enhanced detection and quantification in various biological assays, contributing to a deeper understanding of IP receptor-mediated pathways.
  7. Stable Isotope

    13,14-Dihydro-15-keto Prostaglandin F2α-d4 is a deuterated analog of 13,14-Dihydro-15-keto Prostaglandin F2α, functioning as a stable isotope. This compound is an endogenous metabolite found in blood, making it a valuable tool for investigating biological processes related to pregnancy. It can facilitate quantitative assays and metabolic studies in reproductive biology, enhancing research on prostaglandin metabolism and its implications in gestational health.
  8. Stable Isotope

    Prostaglandin E1-d4 is the deuterium-labeled derivative of Prostaglandin E1, a potent prostanoid receptor ligand. It demonstrates affinity for various prostaglandin receptors, including EP3 and EP4, with inhibition constants of 1.1 nM and 2.1 nM, respectively. This compound plays a critical role in inducing vasodilation and inhibiting platelet aggregation, making it a valuable tool for research applications in cardiovascular health and peripheral vascular diseases. Prostaglandin E1-d4 can facilitate advanced studies of prostanoid signaling pathways and therapeutic interventions.
  9. Stable Isotope

    MRE-269-d7 sodium is a deuterium-labeled analog of MRE-269, serving as a stable isotope for research. This reagent retains the biological activity of MRE-269, which modulates specific signaling pathways. It is primarily utilized in pharmacokinetic studies and metabolic research to track and quantify metabolites, facilitating understanding of drug metabolism and disposition.
  10. Stable Isotope

    Tetranor-PGDM-d6 is a deuterium-labeled analog of Tetranor-PGDM, serving as a stable isotope tracer. This compound is pivotal for metabolic studies and analytical applications in biological research. Its incorporation into various assays enhances the understanding of cellular pathways and lipid metabolism, facilitating detailed investigations into physiological processes.
  11. Stable Isotope

    13,14-Dihydro-15-keto prostaglandin D2-d9 is a deuterium-labeled derivative of 13,14-Dihydro-15-keto prostaglandin D2, which acts as a selective agonist for the DP2 receptor. This compound is a key metabolite produced via the 15-hydroxyl PGDH pathway and is valuable for studying prostaglandin signaling. Its ability to inhibit ion flux in canine colonic mucosa makes it pertinent for gastrointestinal and inflammation research applications.
  12. Stable Isotope

    3-epi-Calcifediol is the C-3 epimer of 25-hydroxy vitamin D3, acting as a stable isotope for research applications. This compound has been shown to reduce serum parathyroid hormone (PTH) levels in male weanling rats when administered dietary doses of 0.5 and 1 IU/g, suggesting its potential role in calcium regulation and bone metabolism studies. Its unique properties make it a valuable tool for investigating the biological effects of vitamin D metabolism.
  13. Stable Isotope

    6β-Naltrexol-d3 is a deuterium-labeled form of 6β-Naltrexol, a potent peripherally selective opioid antagonist derived from Naltrexone. This compound selectively inhibits gastrointestinal opioid effects, making it useful in the study of opioid receptor functionality and gastrointestinal motility. Research applications include investigating the modulation of opioid effects on gastrointestinal transit and exploring potential therapeutic strategies for opioid-induced constipation.
  14. Isotope-Labeled Compound

    O-Desmethyl Tramadol-d6 is a deuterium-labeled derivative of O-Desmethyl Tramadol, which acts primarily as an active metabolite of Tramadol. It is known to exert its analgesic effects through selective interaction with the μ-opioid receptor. This compound serves as a valuable tool in pharmacokinetic studies and metabolic research, particularly in elucidating the metabolic pathways involving cytochrome P450 (CYP) 2D6 enzyme activity.
  15. Stable Isotope

    Naltrexone-d4 is a deuterated analogue of Naltrexone, serving as a stable isotope used in metabolic and pharmacokinetic studies. Its primary mechanism involves antagonism of opioid receptors, making it valuable in researching opioid receptor dynamics and the pharmacological profiles of opioid-related compounds. This reagent is essential for studies requiring precise isotopic labeling and tracing in biological systems, enhancing the understanding of drug metabolism and interactions.
  16. Stable Isotope

    Alvimopan-d7 is a deuterium-labeled variant of Alvimopan, a potent and selective oral μ-opioid receptor antagonist. With an IC50 of 1.7 nM, Alvimopan exhibits significant selectivity for the μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors, with Kis of 100 nM and 12 nM, respectively. This stable isotope-labeled compound is valuable for research applications focused on postoperative ileus and opioid receptor pharmacology.
  17. Isotope-Labeled Compound

    O,O-Diethyl dithiophosphate-13C4 ammonium is a stable isotope-labeled compound used primarily in chemical and biological research. It serves as a useful tool for tracing and quantifying metabolic pathways in various biological systems due to its incorporation of the carbon-13 isotope. This compound aids in the study of organophosphate interactions and can enhance the understanding of biochemical mechanisms and environmental fate of similar thiophosphate agents.
  18. Stable Isotope

    O-Desmethyltramadol-d6 hydrochloride is a deuterated stable isotope of O-Desmethyltramadol hydrochloride, the principal active metabolite of tramadol. This compound is capable of traversing the blood-brain barrier and primarily exerts its analgesic effects through activation of the µ-opioid receptor (µ-OR). O-Desmethyltramadol-d6 hydrochloride is valuable in pharmacokinetic studies and tracer research due to its isotopic labeling, offering precise tracking in biological systems.
  19. Stable Isotope

    Ticagrelor-d7 is a deuterium-labeled derivative of Ticagrelor, a reversible P2Y12 receptor antagonist. This stable isotope is utilized in research for studying platelet aggregation and related cardiovascular processes. Its unique labeling enables precise tracking and quantification in various biochemical assays, enhancing the understanding of antiplatelet therapies in clinical and experimental settings.
  20. Stable Isotope

    Prasugrel-d3 is a deuterium-labeled form of Prasugrel, a thienopyridine prodrug that selectively antagonizes the P2Y12 receptor. This compound effectively inhibits ADP-induced platelet aggregation, thereby demonstrating significant platelet-inhibitory activity. Prasugrel-d3 is valuable for studying platelet function and the pharmacokinetics of Prasugrel in various biological research applications.
  21. Stable Isotope

    Uridine 5′-diphosphoglucose-13C6 disodium is a stable isotope-labeled form of Uridine 5′-diphosphoglucose. It functions primarily as a potent agonist of the proinflammatory P2Y14 receptor, playing a crucial role in modulating inflammation and neutrophil polarization. This compound is significant for research applications in understanding cellular responses to ischemia and reperfusion, particularly in myocardial infarction models. Additionally, it serves as a precursor for glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids, making it valuable for various biochemical studies.
  22. Stable Isotope

    Prasugrel-13C6 is a stable isotope-labeled form of Prasugrel, a thienopyridine compound classified as a prodrug. It functions as a potent P2Y12 receptor antagonist, effectively inhibiting ADP-induced platelet aggregation, thereby reducing platelet activation and aggregation in cardiovascular settings. This reagent is valuable for research applications involving pharmacokinetics, metabolism studies, and mechanisms of platelet inhibition.
  23. Stable Isotope

    Clopidogrel-13C,d3 sulfate is a stable isotope-labeled version of (±)-Clopidogrel bisulfate, primarily functioning as a platelet P2Y12 receptor inhibitor and ADP receptor antagonist. It inhibits the binding of adenosine diphosphate (ADP) to its receptors on platelet membranes, thereby blocking ADP-mediated activation of the GPIIb/IIIa complex. This compound demonstrates significant potential in reducing vascular inflammation and attenuating progression of angiotensin II-induced abdominal aortic aneurysms, in addition to exhibiting anti-inflammatory properties. It is utilized in various research applications focused on platelet aggregation and cardiovascular health.
  24. Stable Isotope

    (±)-Clopidogrel-d4 is a deuterium-labeled derivative of (±)-Clopidogrel, a selective platelet P2Y12 receptor inhibitor and adenosine diphosphate (ADP) receptor antagonist. This compound effectively prevents ADP binding to platelet receptors, thereby inhibiting ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel-d4 is utilized in research related to vascular inflammation and the progression of conditions such as angiotensin II-induced abdominal aortic aneurysms, and it also exhibits notable anti-inflammatory properties.
  25. Stable Isotope

    Prasugrel-d4 is a deuterated analog of Prasugrel, a thienopyridine compound that acts as a potent P2Y12 receptor antagonist. By inhibiting ADP-induced platelet aggregation, Prasugrel is utilized in various research applications related to cardiovascular diseases and thrombosis studies. The stable isotope labeling allows for advanced pharmacokinetic and metabolic investigations, facilitating deeper insights into the drug's mechanism of action and its effects on platelet function.
  26. Stable Isotope

    Prasugrel-d5 is a deuterium-labeled variant of Prasugrel, a thienopyridine prodrug that functions as a potent inhibitor of platelet aggregation. By acting as an antagonist of the P2Y12 receptor, Prasugrel-d5 effectively inhibits ADP-induced platelet activation. This stable isotope can be used in pharmacokinetic studies and metabolic profiling to enhance understanding of drug metabolism and therapeutic effects in cardiovascular research.
  27. Stable Isotope

    Clopidogrel-d3 hydrogen sulfate is a deuterated form of Clopidogrel hydrogen sulfate, primarily designed as a stable isotope for pharmacokinetic studies. This compound functions as a potent antiplatelet agent, preventing blood clot formation by inhibiting platelet aggregation induced by ADP. Clopidogrel-d3 hydrogen sulfate also selectively inhibits cytochrome P450 isoforms CYP2B6 and CYP2C19, with IC50 values of 18.2 nM and 524 nM, respectively. Its usage is instrumental in research involving antithrombotic therapies and drug metabolism.
  28. Stable Isotope

    Uridine 5′-diphosphoglucose-13C disodium is a stable isotope-labeled form of Uridine 5′-diphosphoglucose (UDP-glucose). This compound functions as a potent agonist for the proinflammatory P2Y14 receptor, playing a critical role in modulating inflammation and the polarization of neutrophils. Additionally, UDP-glucose is a key precursor for the synthesis of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in both animal tissues and select microorganisms. It holds potential for research applications focused on mitigating inflammation associated with myocardial infarction and reperfusion injury in cardiac tissue.
  29. Stable Isotope

    Ticagrelor-d4 is a deuterium-labeled derivative of Ticagrelor, functioning as a reversible oral P2Y12 receptor antagonist. This stable isotope is primarily utilized in pharmacokinetic and metabolic studies, providing a valuable tool for investigating pharmacodynamics and the pharmacological effects of Ticagrelor. Its application in research facilitates a deeper understanding of platelet aggregation mechanisms and the drug's therapeutic efficacy.
  30. Stable Isotope

    (±)-Clopidogrel-d7 sulfate is a stable isotope-labeled derivative of (±)-Clopidogrel sulfate, featuring deuterium substitution. This compound serves as an important tool in pharmacokinetic studies and drug metabolism research, facilitating the investigation of clopidogrel's biotransformation and biological activity. Its isotopic labeling enables detailed analysis in mass spectrometry applications, providing insights into drug interactions and therapeutic efficacy.
  31. Stable Isotope

    Rac-Fesoterodine-d14 fumarate is a stable isotope-labeled version of the racemic muscarinic receptor antagonist Fesoterodine. It exhibits competitive inhibition across multiple mAChR subtypes, with pKivalues of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This compound is primarily utilized in research applications focusing on the pharmacological characterization and monitoring of overactive bladder treatments.
  32. Stable Isotope

    (R)-Oxybutynin-d10 is a deuterium-labeled derivative of (R)-Oxybutynin, a racemic isomer known for its role as a muscarinic receptor antagonist. This compound exhibits antispasmodic, antimuscarinic, and anticholinergic properties, effectively competing with carbachol-induced contractions. (R)-Oxybutynin-d10 is utilized in research related to urinary incontinence and neurogenic bladder dysfunction, facilitating the study of mechanisms underlying these conditions.
  33. Stable Isotope

    Biperiden-d5 is a deuterium-labeled analog of Biperiden, a non-selective muscarinic receptor antagonist that primarily targets M1 muscarinic receptors. By competitively binding to these receptors, Biperiden-d5 inhibits acetylcholine signaling, which can enhance dopaminergic activity within the central nervous system. This stable isotope is valuable for research applications related to Parkinson's disease and associated neuropsychiatric disorders, providing insights into receptor interactions and signaling pathways.
  34. Stable Isotope

    (1R,3S-)Solifenacin-d5 hydrochloride is a deuterated form of Solifenacin hydrochloride, a potent muscarinic receptor antagonist. It exhibits significant binding affinity with pKis of 7.6, 6.9, and 8.0 for M1, M2, and M3 receptors, respectively. This stable isotope is valuable for use in pharmacokinetic studies and metabolic research, facilitating the investigation of drug metabolism and receptor interactions.
  35. Stable Isotope

    Flavoxate-d4 hydrochloride is a deuterated form of Flavoxate hydrochloride, acting as a muscarinic acetylcholine receptor antagonist. It is utilized in the study of urinary disorders and exhibits antispasmodic properties. This stable isotope is particularly useful in pharmacokinetic studies and metabolic research, enabling precise tracking and quantification of the compound in various biological systems.
  36. Stable Isotope

    (R)-Hydroxytolterodine-d14 is a deuterated form of Desfesoterodine, a selective antagonist of muscarinic acetylcholine receptors (mAChRs). This compound exhibits high potency, with a KB value of 0.84 nM and a pA2 of 9.14. As a significant metabolite of Tolterodine and Fesoterodine, it has demonstrated efficacy in models of cerebral infarction-induced detrusor overactivity in rats, making it valuable for research in urology and neurology.
  37. Stable Isotope

    Ethyl linolenate-d5 is the deuterium-labeled form of Ethyl linolenate, a fatty acid ethyl ester. This compound is known for its ability to inhibit melanin production, demonstrating an IC50 value of 70 μM. It is primarily utilized in research applications focused on melanogenesis and can serve as a valuable tool in studying pigmentation processes and related disorders.
  38. Stable Isotope

    Ramelteon metabolite M-II-d3 is a deuterium-labeled derivative of the major metabolite M-II of Ramelteon, a selective agonist of melatonin receptors (MT1 and MT2). This reagent exhibits significant biological activity, with IC50 values of 208 pM and 1470 pM for human MT1 and MT2 receptors, respectively. It is primarily used in pharmacological studies and metabolic research involving melatonin signaling pathways.
  39. Stable Isotope

    Ramelteon-d5 is a deuterated form of Ramelteon, a highly selective and potent agonist of the MT1 and MT2 melatonin receptors, exhibiting Ki values of 14 pM and 112 pM, respectively. This stable isotope is valuable for research studies focusing on insomnia and sleep disorders, as Ramelteon has demonstrated efficacy in reducing sleep onset during long-term treatment without leading to next-morning residual effects or withdrawal symptoms upon discontinuation. Researchers can utilize Ramelteon-d5 in pharmacokinetic and metabolic studies to gain insights into the compound's mechanism and therapeutic potential.
  40. Stable Isotope

    Tasimelteon-d5 is a deuterium-labeled derivative of Tasimelteon, a selective dual melatonin receptor agonist targeting MT1 and MT2 receptors. This compound exhibits significantly higher affinity for the MT2 receptor, with an affinity range of 2.1-4.4 times greater than that for the MT1 receptor. Tasimelteon serves as a circadian regulator and is being investigated for its potential therapeutic applications in managing Non-24-Hour Sleep-Wake Disorder (Non-24).
  41. Stable Isotope

    Ramelteon-d3 is a deuterium-labeled derivative of Ramelteon, a highly selective and orally active agonist of melatonin receptors MT1 and MT2, exhibiting Ki values of 14 pM and 112 pM, respectively. This stable isotope is utilized in pharmacokinetic studies and research applications focused on insomnia, providing insight into sleep modulation mechanisms. Ramelteon is known for its efficacy in reducing sleep onset without causing residual effects, rebound insomnia, or withdrawal symptoms with long-term use.
  42. Stable Isotope

    O-Phospho-L-serine-13C3,15N is a stable isotope-labeled form of O-Phospho-L-serine, which serves as the immediate precursor to L-serine in the serine biosynthesis pathway. This compound functions as an agonist at group III metabotropic glutamate receptors (mGluR4, mGluR6, mGluR7, and mGluR8) and exhibits weak antagonistic properties at mGluR1 while acting as a potent antagonist at mGluR2. Its unique isotopic labeling makes it valuable for metabolic and neurobiological research, particularly in studies involving neurotransmitter signaling and cellular metabolism.
  43. Stable Isotope

    O-Phospho-L-serine-13C3 is a stable isotope-labeled form of O-Phospho-L-serine, serving as a valuable tool in metabolic studies. As an immediate precursor to L-cysteine in the serine synthesis pathway, it plays a critical role in amino acid metabolism. This compound also acts as an agonist for group III metabotropic glutamate receptors (mGluR4, mGluR6, mGluR7, and mGluR8) while exhibiting weak antagonistic properties at mGluR1 and potent antagonism at mGluR2. Its isotopic labeling makes it suitable for tracing and quantifying metabolic pathways in research applications.
  44. Stable Isotope

    Netupitant-d6 is a deuterated derivative of Netupitant, a highly potent and selective neurokinin-1 (NK1) receptor antagonist. This stable isotope is utilized in various biochemical and pharmacological studies to investigate the mechanisms of action and metabolic pathways of NK1 receptor inhibitors. Its application in research facilitates the analysis of drug behavior, distributions, and interactions within biological systems.
  45. Stable Isotope

    Maropitant-d3 is a deuterium-labeled derivative of Maropitant, a selective neurokinin (NK1) receptor antagonist. This compound functions by inhibiting the binding of substance P in the emetic center and the chemoreceptor trigger zone (CRTZ), showcasing significant efficacy in the prevention of vomiting. Maropitant-d3 is valuable in chemical research requiring stable isotopes for the study of pharmacokinetics and metabolism of NK1 receptor antagonists.
  46. Stable Isotope

    Riociguat-d3 is a deuterium-labeled derivative of Riociguat, a potent oral stimulator of soluble guanylate cyclase (sGC). This stable isotope is utilized primarily in research applications focusing on the pharmacokinetics and metabolic pathways of Riociguat. Its unique labeling allows for advanced analytical studies and enhances understanding of sGC's role in the treatment of pulmonary hypertension.
  47. Stable Isotope

    Leukotriene B4-d4 is a deuterium-labeled analog of Leukotriene B4 (LTB4), a potent chemoattractant for leukocytes that plays a significant role in inflammatory responses. This stable isotope can be utilized in research to trace LTB4 in biological systems, enhancing the understanding of its involvement in various inflammatory diseases. Additionally, LTB4 serves as an alkyl chain-based linker in the development of PROTACs, facilitating targeted protein degradation studies.
  48. Stable Isotope

    Montelukast-d6 sodium is a deuterium-labeled form of Montelukast, a potent and selective oral antagonist of the cysteinyl leukotriene receptor 1 (Cysltr1). This reagent is crucial for research applications focused on asthma and liver injury, offering insights into leukotriene signaling pathways. Additionally, Montelukast-d6 sodium exhibits antioxidant properties, making it relevant for studies on intestinal ischemia-reperfusion injury and the mitigation of cardiac damage.
  49. Stable Isotope

    Montelukast-d6 is a deuterated form of Montelukast, a selective antagonist of the cysteinyl leukotriene receptor 1 (CysLTR1). This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Montelukast, particularly in the contexts of asthma and liver injury. Additionally, Montelukast has demonstrated antioxidant properties in models of intestinal ischemia-reperfusion injury and has potential applications in studying cardiac damage.
  50. Stable Isotope

    Pranlukast-d4 is a deuterated form of Pranlukast, which selectively and competitively antagonizes peptide leukotrienes. This stable isotope demonstrates high potency in inhibiting bindings of [3H]LTE4, [3H]LTD4, and [3H]LTC4 to lung membranes, with inhibition constants of 0.63±0.11 nM, 0.99±0.19 nM, and 5640±680 nM, respectively. Pranlukast-d4 is valuable for pharmacokinetic studies and metabolic profiling in research related to asthma and allergic conditions.

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