Isotope-Labeled Compounds

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  1. Stable Isotope

    Tamsulosin-d4 hydrochloride is a deuterium-labeled derivative of Tamsulosin, a selective α1-adrenergic receptor inhibitor. This stable isotope is utilized in pharmacokinetic studies and metabolic research related to prostatic hyperplasia. Additionally, Tamsulosin has demonstrated effects in attenuating the growth of abdominal aortic aneurysms in experimental models, making it relevant for studies in vascular biology and urology.
  2. Stable Isotope

    Alfuzosin-d7 is a deuterium-labeled form of Alfuzosin, a selective and competitive antagonist of the α1-adrenoceptor. This compound effectively relaxes smooth muscle in the prostate and bladder neck, facilitating improved urination. Alfuzosin-d7 serves as a stable isotope for quantitative analysis and is useful in research on benign prostatic hyperplasia (BPH).
  3. Stable?Isotope

    Droxidopa-13C2,15N hydrochloride is a stable isotope-labeled variant of Droxidopa. As a prodrug, Droxidopa acts as a precursor to norepinephrine and epinephrine, facilitating their synthesis. This compound is notable for its ability to cross the blood-brain barrier, making it useful in neurological research and studies focused on neurotransmitter function and pharmacodynamics. The stable isotopes provide valuable tools for tracing and quantifying biochemical pathways in various biological systems.
  4. Stable Isotope

    (Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies.
  5. Stable Isotope

    Isoprenaline-d7 hydrochloride is a deuterated analog of Isoprenaline, serving as a stable isotope for research applications. As a non-selective β-adrenergic receptor agonist, Isoprenaline exhibits significant peripheral vasodilatory, bronchodilator, and cardiac stimulatory effects. This compound is valuable for studying conditions such as bradycardia and bronchial asthma, providing insights into β-adrenergic signaling pathways and related therapeutic interventions.
  6. Stable Isotope

    4-Hydroxypropranolol-d7 is a deuterium-labeled derivative of the active metabolite 4-Hydroxypropranolol hydrochloride, which targets β1- and β2-adrenergic receptors with high affinity, exhibiting pA2 values of 8.24 and 8.26, respectively. This compound maintains comparable potency to Propranolol and displays intrinsic sympathomimetic activity, membrane-stabilizing properties, and potent antioxidant effects. 4-Hydroxypropranolol-d7 is instrumental for pharmacokinetic studies, providing valuable insights into drug metabolism and receptor activity in various biological assays.
  7. Isotope-Labeled Compound

    0
  8. Stable Isotope

    Ractopamine-d6 hydrochloride is a deuterium-labeled derivative of Ractopamine, a potent β-adrenergic receptor (βAR) agonist, exhibiting binding affinities of approximately 25 nM for both pig β1AR and β2AR. This stable isotope compound is primarily utilized in research focused on protein metabolism, particularly in enhancing lean tissue growth and improving production efficiency in swine. Its applications extend to studies investigating the physiological effects and benefits of βAR modulation in livestock management.
  9. Stable Isotope

    Colterol hydrochloride-d9 is a deuterium-labeled derivative of Colterol hydrochloride, a selective agonist for adrenergic receptors. It demonstrates significant binding affinity for both the β1-adrenoreceptor, with an IC50 of 645 nM, and the β2-adrenoreceptor, with an IC50 of 147 nM. This compound is primarily utilized in research focusing on adrenergic signaling and has potential applications as a bronchodilator in respiratory studies.
  10. Stable Isotope

    Medetomidine-d5 (d5-Major) is a deuterium-labeled derivative of Medetomidine, a potent α2-adrenoceptor agonist with a Ki value of 1.08 nM. This compound exhibits sedative and analgesic properties, making it valuable in research focused on anesthetic and pain management applications. Additionally, Medetomidine's activation of α2-adrenoceptors leads to peripheral vasoconstriction, further expanding its potential uses in studying cardiovascular responses and drug interactions.
  11. Stable Isotope

    Carazolol-d7 is a stable isotope form of Carazolol, a highly potent antagonist of β1 and β2 adrenoceptors. Additionally, Carazolol acts as a selective agonist for the β3-adrenoceptor, making it a valuable compound in studies of adrenergic receptor pharmacology. This reagent is particularly useful in hypertension research, enabling researchers to explore mechanisms of action and receptor interactions in cardiovascular studies.
  12. Stable Isotope

    Ractopamine-13C2 is a stable isotope-labeled version of Ractopamine, a potent β-adrenergic receptor agonist. With a Kd of approximately 25 nM for both pig β1 and β2 adrenergic receptors, Ractopamine is also an mTAAR1 agonist characterized by an EC50 of 16 μM. This compound enhances muscle mass development while minimizing fat deposition, resulting in improved growth rates and feed efficiency in swine. Ractopamine-13C2 is ideal for research focused on optimizing lean tissue growth and production efficiency in livestock.
  13. Stable Isotope

    Practolol-d7 is the deuterated form of Practolol, a selective antagonist of the β1-adrenergic receptor. This stable isotope is invaluable for pharmacokinetic studies and metabolic research involving β1-adrenergic signaling pathways. Practolol-d7 is useful in the investigation of cardiac arrhythmias and potential therapeutic interventions targeting these conditions.
  14. Stable Isotope

    Phenoxybenzamine-d5 is a deuterium labeled derivative of Phenoxybenzamine, a nonselective, irreversible α-adrenoceptor antagonist. This compound is primarily utilized in research focused on hypertension, including conditions such as pheochromocytoma. In addition to its cardiovascular applications, Phenoxybenzamine exhibits antitumor properties, making it valuable for studies in oncology and related fields.
  15. Stable Isotope

    Cimbuterol-d9 is a deuterium-labeled derivative of Cimbuterol, functioning as a β-adrenergic agonist. This compound targets β-adrenergic receptors, exhibiting significant bronchodilator and tocolytic properties. Its stable isotope incorporation facilitates advanced pharmacokinetic studies and metabolic research applications, allowing for more precise investigations into the growth-promoting effects of β-adrenergic agonists.
  16. Stable Isotope

    Clorprenaline-d6 is a deuterated form of Clorprenaline, serving as a stable isotope for metabolic and pharmacokinetic studies. This compound retains the pharmacological properties of its non-deuterated counterpart, enabling researchers to investigate the metabolism and distribution of Clorprenaline in biological systems. Clorprenaline-d6 is valuable for studies involving adrenergic agonists and can aid in the development of novel therapeutic agents.
  17. Stable Isotope

    Phenylethanolamine A-d3 is a deuterium-labeled analogue of Phenylethanolamine A, which functions as a β-adrenergic agonist. This stable isotope is primarily utilized in metabolic studies and pharmacokinetic research to trace and quantify drug behavior in biological systems. It serves as a valuable tool for investigating the mechanisms of action and physiological effects associated with β-adrenergic receptor engagement. Additionally, Phenylethanolamine A is a byproduct of Ractopamine synthesis, highlighting its relevance in both metabolic and synthetic research.
  18. Stable Isotope

    Sotalol-d6 is a deuterium-labeled derivative of Sotalol, a non-selective β-adrenergic receptor antagonist. This compound exhibits potent antiarrhythmic activity, making it valuable for studying pediatric arrhythmias. Additionally, Sotalol-d6 inhibits β-receptors and potassium KCNH2 channels, highlighting its utility in the investigation of cardiac electrophysiology and as a potential antiepileptic agent.
  19. Stable Isotope

    Betaxolol-d5 is a deuterated form of Betaxolol, a selective beta-1 adrenergic receptor antagonist. This stable isotope is primarily utilized in pharmacokinetic studies to investigate hypertension and glaucoma treatment mechanisms. The use of Betaxolol-d5 allows for enhanced studies on drug metabolism, distribution, and elimination in various biological contexts.
  20. Stable Isotope

    DL-Norepinephrine-d3 hydrochloride is a deuterium-labeled form of the racemic catecholamine neurotransmitter, DL-Norepinephrine hydrochloride. This compound serves as a stable isotope tracer, facilitating research applications in neuropharmacology and neurobiology. It enables the study of neurotransmitter dynamics and receptor interactions, contributing valuable insights into conditions such as Parkinson's disease. Researchers can utilize DL-Norepinephrine-d3 hydrochloride to explore pathways associated with catecholamine signaling and its implications in neurological disorders.
  21. Stable Isotope

    (±)-Penbutolol-d9 hydrochloride is a deuterated derivative of (±)-Penbutolol hydrochloride, a selective β-adrenoceptor antagonist. This compound exhibits a reported IC50 of 0.74 μM, demonstrating its potency in modulating β-adrenoceptor activity. It is primarily utilized in pharmacological research to investigate receptor dynamics and bioavailability of β-blockers in various biological systems.
  22. Stable Isotope

    Phenylephrine-d3 hydrochloride is a deuterium-labeled analogue of Phenylephrine hydrochloride, serving as a stable isotope. As a selective α1-adrenoceptor agonist, it exhibits potent activity with pKis of 5.86 for α1D, 4.87 for α1B, and 4.70 for α1A receptors. This reagent is valuable for research involving receptor-ligand interactions and pharmacokinetic studies, enabling precise measurement and analysis in various biological settings.
  23. Stable Isotope

    Ractopamine-d5 hydrochloride is a stable isotope-labeled form of the potent β-adrenergic receptor (βAR) agonist, Ractopamine hydrochloride. It exhibits strong binding affinity to pig β1AR and β2AR, with Kd values approximately 25 nM. This reagent is primarily utilized in research focused on protein metabolism, specifically for studying the enhancement of lean tissue growth and production efficiency in swine.
  24. Stable Isotope

    (R)-Carvedilol-d4 is a deuterium-labeled derivative of (R)-Carvedilol, primarily targeting α-adrenergic receptors. This compound exhibits significant biological activity by inhibiting spontaneous Ca2+ waves and effectively mitigating stress-induced ventricular tachycardia. Furthermore, (R)-Carvedilol-d4 demonstrates potential in research applications related to cardiovascular health and oncology, notably delaying the progression of UV-induced skin tumors and reducing their malignancy.
  25. Stable Isotope

    Clonidine-d4 is a deuterated form of Clonidine, serving as a stable isotope. Its primary mechanism targets the α2-adrenoceptors, functioning as a potent antihypertensive agent. Clonidine-d4 is valuable for pharmacokinetic studies and tracer applications in metabolic experiments, allowing for precise quantification and analysis in research settings.
  26. Stable Isotope

    DL-Phenylephrine-d3 hydrochloride is a deuterium-labeled derivative of DL-Phenylephrine hydrochloride, primarily targeting the alpha1-adrenergic receptor. This compound demonstrates significant vasoconstrictive activity, making it useful in the study of adrenergic signaling pathways. Its stable isotope labeling facilitates precise quantitative analyses in pharmacokinetic studies and metabolic research applications.
  27. Stable Isotope

    Phenylephrine-d6 hydrochloride is a deuterated form of Phenylephrine, serving as a stable isotope used in chemical research. It functions primarily as a selective α1-adrenoceptor agonist, exhibiting pKis of 5.86, 4.87, and 4.70 for α1D, α1B, and α1A receptor subtypes, respectively. This reagent is valuable for studies investigating adrenergic signaling and receptor pharmacology, offering insights into cardiovascular and neurophysiological pathways.
  28. Stable Isotope

    Bisoprolol-d7 is a deuterium-labeled analog of Bisoprolol, a selective and orally active β1-adrenergic receptor blocker with minimal β2-receptor activity. This stable isotope is primarily used in pharmacokinetic studies to investigate the metabolism and distribution of Bisoprolol in biological systems. Its applications extend to research involving hypertension, coronary artery disease, and stable ventricular dysfunction.
  29. Stable Isotope

    Salmeterol-d5 is a deuterated analog of Salmeterol, serving as a stable isotope. Salmeterol is a highly selective agonist of the human β2 adrenergic receptor, demonstrating significant stimulation of cAMP accumulation in Chinese Hamster Ovary (CHO) cells expressing β2, β1, and β3 adrenoceptors with pEC50 values of 9.6, 6.1, and 5.9, respectively. This compound is valuable in pharmacological research, particularly in studies investigating β2 adrenergic signaling pathways and respiratory system pharmacotherapy.
  30. Stable Isotope

    Zilpaterol-d7 is a deuterium-labeled variant of Zilpaterol, a selective β-adrenergic agonist. This stable isotope serves as a valuable tool in research involving metabolic studies and pharmacokinetics, particularly in livestock applications. Its use can facilitate investigations into the specific metabolic pathways affected by β-agonists in animal nutrition and performance.
  31. Stable Isotope

    Betaxolol-d7 hydrochloride is a deuterium-labeled analog of Betaxolol hydrochloride, functioning primarily as a selective beta-1 adrenergic receptor blocker. This stable isotope is instrumental in pharmacokinetic studies and metabolic investigations, particularly in the context of hypertension and glaucoma research. Its unique labeling enables precise tracking and quantification in various biological assays, facilitating advanced research into cardiovascular and ocular conditions.
  32. Stable Isotope

    Ractopamine-d6 is a deuterium-labeled analogue of Ractopamine, a potent β-adrenergic receptor (βAR) agonist with a Kd of approximately 25 nM for both pig β1AR and β2AR. This stable isotope enables detailed studies of protein metabolism and is instrumental in research focused on enhancing lean tissue growth and improving production efficiency in swine. Its application is crucial for understanding the biochemical pathways influenced by β-adrenergic signaling in agricultural and animal health settings.
  33. Stable Isotope

    Guanfacine-13C,15N3 is a stable isotope-labeled form of Guanfacine, an orally active noradrenergic α2A adrenergic receptor agonist. This compound exhibits high selectivity for the α2A receptor subtype, contributing to its pharmacological effects such as hypotension and sedation. Guanfacine-13C,15N3 serves as a valuable tool in research applications focused on prefrontal cortex cognitive disorders, including Tourette's syndrome and attention deficit hyperactivity disorder (ADHD).
  34. Stable Isotope

    Paroxetine-d6-1 is a deuterated derivative of Paroxetine, a potent and selective serotonin reuptake inhibitor (SSRI). Primarily, it targets the serotonin transporter, displaying minimal activity as a norepinephrine uptake inhibitor. This stable isotope-labeled reagent is valuable for pharmacokinetic studies, drug metabolism research, and the investigation of SSRIs' mechanism of action.
  35. Stable Isotope

    Meclofenamic acid-d4 is the deuterium-labeled analog of Meclofenamic acid, a non-steroidal anti-inflammatory drug. This compound functions primarily as a selective inhibitor of the fat mass and obesity-associated (FTO) enzyme by competing for its binding to m(6)A-containing nucleic acids. Additionally, Meclofenamic acid exhibits non-selective gap-junction blocking activity, making it valuable for studies in cellular communication and metabolic regulation. Its isotopic labeling enhances its utility in various analytical approaches in chemical biology research.
  36. Stable Isotope

    Tonabersat-d6 (SB-220453-d6) is a deuterated form of Tonabersat, a potent gap-junction modulator. This compound has been demonstrated to reduce inflammatory damage in the central nervous system, making it an important tool for research in neuroprotection and neuroinflammation. Tonabersat-d6 can be utilized in studies requiring stable isotope labeling for metabolic tracking or mechanistic investigations of gap-junction communications in various cellular contexts.
  37. Stable Isotope

    Tirofiban-d9 is a deuterium-labeled analogue of Tirofiban, a potent platelet glycoprotein IIb/IIIa inhibitor. This stable isotope can be utilized in pharmacokinetic studies, enabling researchers to investigate the metabolism and distribution of Tirofiban in biological systems. Its design provides enhanced specificity and sensitivity in analytical applications, facilitating a deeper understanding of its pharmacological effects.
  38. Stable Isotope

    Mavacamten-d5 is a deuterated derivative of Mavacamten, specifically designed as a stable isotope for research applications. Mavacamten functions as an orally active modulator of cardiac myosin, displaying IC50 values of 490 nM and 711 nM for bovine and human cardiac myosin, respectively. This compound is utilized in biochemical studies to explore cardiac function and the modulation of myosin activity in heart diseases.
  39. Stable Isotope

    Danicamtiv-d6 is a deuterated variant of Danicamtiv, an inotropic agent that selectively activates cardiac myosin through allosteric modulation. This compound enhances cardiac systolic function while maintaining mechanical efficiency, making it valuable for studying cardiac physiology. Danicamtiv-d6 is suitable for research applications that require stable isotope labeling in metabolic studies and pharmacological investigations of cardiac function.
  40. Stable Isotope

    Danicamtiv-d3 is a deuterated labeled version of the inotropic agent Danicamtiv (MYK-491), targeting cardiac myosin as a selective allosteric activator. This compound enhances cardiac systolic function while maintaining mechanical efficiency, making it valuable for research into heart function and therapies for heart failure. Its stable isotope composition allows for advanced analytical techniques, providing insights into the dynamics of cardiac contractility.
  41. Stable Isotope

    Mavacamten-d6 is a deuterium-labeled analog of Mavacamten, a selective modulator of cardiac myosin. It demonstrates inhibitory activity with IC50 values of 490 nM for bovine cardiac myosin and 711 nM for human cardiac myosin. This stable isotope form is useful in pharmacokinetic studies and metabolic research to trace and quantify drug behavior in biological systems.
  42. Stable Isotope

    Mavacamten-d1 is a deuterium-labeled derivative of Mavacamten, a selective modulator of cardiac myosin that interacts with myosin to reduce cardiac contractility. This compound exhibits significant inhibitory activity with IC50 values of 490 nM for bovine cardiac myosin and 711 nM for human cardiac myosin. Mavacamten-d1 is valuable for metabolic studies, pharmacokinetic assessments, and other research applications requiring stable isotopes in cardiac function investigations.
  43. Stable Isotope

    Bempedoic acid-d5 is a deuterium-labeled analogue of Bempedoic acid, an ATP-citrate lyase (ACL) inhibitor. This compound plays a significant role in the activation of AMP-activated protein kinase (AMPK), which is crucial for regulating energy metabolism. Bempedoic acid-d5 is valuable for applications in metabolic research, facilitating studies on dyslipidemia and cardiometabolic diseases.
  44. Stable Isotope

    5-Methyl-2'-deoxycytidine-d3 is a deuterium-labeled form of the endogenous DNA methylation marker, 5-Methyl-2'-deoxycytidine. This stable isotope serves as a substrate for DNA methyltransferases, facilitating the regulation of DNA methylation patterns by guiding de novo methylation and activating adjacent CpG site methylation. In addition, 5-Methyl-2'-deoxycytidine-d3 plays a critical role in chromatin dynamics and gene expression, as it influences the recruitment of methyltransferases to specific chromatin regions. Its methylation status is essential for understanding cellular processes related to proliferation and differentiation in various biological contexts.
  45. Stable Isotope

    Levetiracetam-d6 is a deuterium-labeled form of Levetiracetam, an anticonvulsant that targets the synaptic vesicle protein SV2A. This stable isotope is utilized in research to study the pharmacokinetics and dynamics of Levetiracetam. It enhances the efficacy of Temozolomide in glioblastoma stem cells by promoting apoptosis and inhibiting MGMT through modulation of HDAC levels, thus serving as a potential chemosensitizer in cancer therapies.
  46. Stable Isotope

    Levetiracetam-d3 is a deuterated form of Levetiracetam, primarily targeting the synaptic vesicle protein SV2A. This antiepileptic compound enhances the efficacy of Temozolomide by promoting apoptosis and inhibiting the proliferation of glioblastoma stem cells. Levetiracetam-d3 also modulates histone deacetylase (HDAC) levels, leading to the silencing of MGMT and thereby increasing the sensitivity of cancer cells to Temozolomide treatment. This reagent is valuable for chemical research applications related to cancer therapy and neuropharmacology.
  47. Stable Isotope

    Inosine-2,8-d2 is a stable isotope-labeled derivative of inosine, an endogenous purine nucleoside derived from adenosine catabolism. This compound exhibits significant biological activities, including anti-inflammatory, antinociceptive, immunomodulatory, and neuroprotective effects. Its role as an agonist for adenosine A1 and A2A receptors makes it valuable for research applications in neurobiology, immunology, and inflammation studies.
  48. Stable Isotope

    Theobromine-d3 is a deuterium-labeled derivative of Theobromine, a methylxanthine naturally occurring in cacao beans. This stable isotope serves as a valuable tool for studying adenosine receptor A1 (AR1) signaling inhibition in research applications. Theobromine-d3 is essential for metabolic tracing, pharmacokinetic studies, and the exploration of purinergic signaling pathways.
  49. Stable Isotope

    Istradefylline-13C,d3 is a stable isotope-labeled version of Istradefylline, a highly potent and selective antagonist of the adenosine A2A receptor. With a Ki value of 2.2 nM, it demonstrates significant efficacy in experimental models of Parkinson's disease. This reagent is essential for studies involving receptor binding and pharmacokinetics, providing insights into the role of adenosine receptors in neurological disorders.
  50. Stable Isotope

    Theobromine-d6 is a deuterium-labeled derivative of theobromine, a methylxanthine compound primarily found in cacao beans. This isotopically enriched reagent can be utilized in studies focusing on adenosine receptor A1 (AR1) signaling inhibition. It is suitable for quantitative analysis in metabolic studies and the investigation of the pharmacokinetics of theobromine and related compounds.

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