Isotope-Labeled Compounds

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  1. Stable Isotope

    D-erythro-Sphingosine-13C2,d2 is a deuterated analog of D-erythro-Sphingosine, which serves as a stable isotope standard. This compound is a potent activator of p32-kinase with an EC50 of 8 μM and has been shown to inhibit protein kinase C (PKC). Additionally, D-erythro-Sphingosine is recognized as an activator of protein phosphatase 2A (PP2A), making it valuable for studies involving cellular signaling pathways and lipid metabolism.
  2. Stable Isotope

    Niclosamide-13C6 is a stable isotope-labeled form of Niclosamide, a chlorinated salicylanilide known for its anthelmintic properties and potential antitumor activity. This compound functions primarily by inhibiting the Signal Transducer and Activator of Transcription 3 (STAT3) with an IC50 of 0.25 μM in HeLa cells, subsequently affecting DNA replication in vitro. Niclosamide-13C6 is useful in biological studies that require isotope tracking and quantification of drug metabolism and efficacy in cancer research.
  3. Stable Isotope

    Cycloguanil-d4 (hydrochloride) is a deuterium-labeled derivative of Cycloguanil, serving as a stable isotope for research applications. This compound functions as a dihydrofolate reductase (DHFR) inhibitor, with an IC50 of 10.8 μM against human DHFR, and effectively disrupts the folate metabolic pathway, which is critical for nucleotide synthesis and DNA replication. Cycloguanil-d4 is utilized in malaria research due to its ability to inhibit DHFR in Plasmodium species and is also recognized for its potential anticancer activities, as it inhibits DHFR in human cancer cells and blocks transcriptional activity of STAT3.
  4. Stable Isotope

    Cycloguanil-d6 (hydrochloride) is a deuterium-labeled derivative of Cycloguanil, a potent inhibitor of dihydrofolate reductase (DHFR). With an IC50 of 10.8 μM against human DHFR, this stable isotope disrupts the folate metabolic pathway, leading to impaired nucleotide synthesis and DNA replication. Cycloguanil-d6 (hydrochloride) is utilized in malaria research due to its efficacy against Plasmodium DHFR, and it demonstrates significant potential in cancer research by inhibiting DHFR in human cancer cells and blocking STAT3 transcriptional activity.
  5. Stable Isotope

    Niclosamide-13C6 monohydrate is a stable isotope-labeled form of Niclosamide, an orally active antihelminthic agent. This compound functions as a STAT3 inhibitor, exhibiting an IC50 of 0.25 μM in HeLa cells. Niclosamide-13C6 monohydrate demonstrates significant biological activity against various cancer types and has been shown to inhibit DNA replication in Vero E6 cells, making it valuable for research in cancer biology and parasitology.
  6. Stable Isotope

    Nifuroxazide-d4 is a deuterated isotope of Nifuroxazide, a known inhibitor of the transcription factor STAT3. This compound demonstrates significant anti-tumor and anti-metastatic properties, making it valuable for studies investigating cancer biology and therapeutic efficacy. Its stable isotope labeling allows for enhanced tracking and analysis in metabolic and pharmacokinetic research applications.
  7. Stable Isotope

    Pimozide-d5 is a stable isotope-labeled form of Pimozide, a potent antagonist of dopamine receptors primarily targeting D2, D3, and D1 receptors with Ki values of 1.4 nM, 2.5 nM, and 588 nM, respectively. This compound also exhibits affinity for the α1-adrenoceptor with a Ki of 39 nM and has been shown to inhibit signaling pathways through STAT3 and STAT5. Pimozide-d5 is valuable in pharmacological studies and research involving dopamine signaling and receptor interaction.
  8. Stable Isotope

    Pimozide-d5 N-Oxide is a deuterium-labeled derivative of Pimozide, which primarily functions as a dopamine receptor antagonist, exhibiting Ki values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. Additionally, this compound has notable affinity for the α1-adrenoceptor with a Ki of 39 nM. Pimozide also inhibits the signaling pathways of STAT3 and STAT5, making it relevant for research applications in neurobiology and cancer biology studies.
  9. Stable Isotope

    Niclosamide-d3 is a deuterium-labeled derivative of Niclosamide, primarily functioning as a stable isotope. This compound serves as an orally active antihelminthic agent and is extensively utilized in research related to parasitic infections. Additionally, Niclosamide demonstrates significant biological activity as a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells, and has been shown to inhibit DNA replication in Vero E6 cells, making it a valuable tool in cancer research applications.
  10. Stable Isotope

    Pyridoxal Phosphate-d3 is a deuterium-labeled form of Pyridoxal 5'-phosphate, serving as a stable isotope. As the active form of vitamin B6, it acts as a vital cofactor for various enzymes, notably aromatic l-amino acid decarboxylase, which is crucial in synthesizing the neurotransmitters dopamine and serotonin. This compound plays a significant role in vitamin B6 intracellular phosphorylation and interconverts with other coenzyme forms, such as pyridoxine 5'-phosphate and pyridoxamine 5'-phosphate, making it valuable for biochemical and metabolic research applications.
  11. Stable Isotope

    trans-Zeatin-d5 is a deuterium-labeled derivative of trans-Zeatin, a crucial plant cytokinin. It is involved in regulating cell growth, differentiation, and division, thereby influencing a wide range of physiological processes in plants. Additionally, trans-Zeatin has been shown to inhibit UV-induced MEK/ERK activation, making it a valuable reagent for studies in plant biology and related areas of cellular signaling. This stable isotope-labeled compound is useful for tracing and quantifying trans-Zeatin in various biological systems.
  12. Stable Isotope

    Sitagliptin-d4 phosphate is a deuterium-labeled derivative of Sitagliptin phosphate, a selective inhibitor of dipeptidyl peptidase-4 (DPP4) with an IC50 value of 19 nM. This compound increases the levels of active incretins by inhibiting the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Additionally, Sitagliptin-d4 phosphate can stimulate GLP-1 secretion from intestinal L cells through the activation of the cAMP/PKA and ERK1/2 pathways, independent of DPP-4. This reagent is valuable for research into type 1 and type 2 diabetes and can contribute to studies exploring pancreatic islet function.
  13. Stable Isotope

    Pregnenolone-d4-1 is a deuterium-labeled derivative of pregnenolone, a key neurosteroid and precursor to steroid hormones, including steroid ketones. It selectively inhibits cannabinoid CB1 receptors, counteracting the effects of tetrahydrocannabinol (THC) and providing potential neuroprotective benefits against cannabis intoxication. Additionally, pregnenolone-d4-1 activates TRPM3 channels and may exhibit weak activation of TRPM1 channels, making it useful in research related to neurobiology and cannabinoid signaling pathways.
  14. Stable Isotope

    Carvedilol-d4 is a deuterated derivative of Carvedilol, a non-selective β/α-1 adrenergic receptor antagonist. It exhibits dose-dependent inhibition of lipid peroxidation with an IC50 value of 5 μM. Carvedilol acts as a multifaceted antihypertensive agent, demonstrating potential therapeutic applications in managing conditions such as angina and congestive heart failure. Additionally, it has been identified as an autophagy inducer and a modulator of the NLRP3 inflammasome, making it a valuable tool for research into cardiovascular and inflammatory diseases.
  15. Stable Isotope

    Tigecycline-d9 is a deuterium-labeled derivative of the broad-spectrum glycylcycline antibiotic Tigecycline. The compound retains its inhibitory activity against various bacterial strains, demonstrating a mean inhibitory concentration (MIC) of approximately 125 ng/mL for E. coli (MG1655 strain) and MIC50 and MIC90 values of 1 and 2 mg/L for Acinetobacter baumannii, respectively. Tigecycline-d9 is primarily utilized as a stable isotope for research applications in microbiology and antibiotic resistance studies.
  16. Stable Isotope

    Atorvastatin-d5 hemicalcium is a deuterium-labeled derivative of Atorvastatin, functioning primarily as an HMG-CoA reductase inhibitor. This compound effectively reduces blood lipid levels and demonstrates significant biological activity by inhibiting the proliferation and invasion of human vascular smooth muscle cells, with IC50 values of 0.39 μM and 2.39 μM, respectively. It serves as a valuable tool for research applications focused on lipid metabolism and cardiovascular diseases.
  17. Stable Isotope

    Lumefantrine-d9 is a deuterium-labeled variant of Lumefantrine, an established antimalarial agent. This stable isotope serves as a valuable tool for pharmacokinetic studies and metabolic research, particularly in understanding the dynamics of artemether-lumefantrine (AL) combinations in therapeutic applications. Its incorporation in research facilitates the investigation of drug efficacy and metabolism in both preclinical and clinical settings.
  18. Stable Isotope

    Chenodeoxycholic acid-d5 is a deuterium-labeled derivative of Chenodeoxycholic Acid, a hydrophobic primary bile acid. This compound primarily activates the farnesoid X receptor (FXR), a critical nuclear receptor implicated in the regulation of cholesterol metabolism. Chenodeoxycholic acid-d5 is valuable for research applications involving metabolism, bile acid signaling, and nuclear receptor activation studies.
  19. Stable Isotope

    Tolbutamide-d9 is a deuterated form of Tolbutamide, which primarily targets ATP-sensitive potassium channels. As a first-generation sulfonylurea, it functions as an oral hypoglycemic agent, playing a critical role in glucose regulation. This stable isotope is valuable for metabolic research and isotopic tracing studies, facilitating investigations into pharmacokinetics and the mechanism of action of sulfonylureas.
  20. Stable Isotope

    3-Methyladenine-d3 is a deuterium-labeled analog of 3-Methyladenine, a potent inhibitor of phosphoinositide 3-kinase (PI3K). This compound effectively inhibits autophagy by targeting class III PI3K, making it a valuable tool for studying autophagic processes. 3-Methyladenine-d3 is particularly useful in research applications focusing on cellular metabolism, cancer biology, and neurodegenerative diseases where autophagy plays a crucial role.
  21. Stable Isotope

    Omeprazole-d3 is a deuterium-labeled variant of Omeprazole, a widely used proton pump inhibitor (PPI) targeting gastric acid secretion. It demonstrates competitive inhibition of CYP2C19 with an inhibition constant (Ki) between 2 to 6 μM, and has been shown to inhibit the growth of both Gram-positive and Gram-negative bacteria. This stable isotope is particularly useful for pharmacokinetic studies, metabolic profiling, and investigations into drug-drug interactions involving Omeprazole.
  22. Stable Isotope

    Ambroxol-d5 hydrochloride is the deuterium-labeled derivative of Ambroxol hydrochloride, which functions as a glucocerebrosidase (GCase) chaperone. It enhances GCase activity and exhibits potent expectorant properties. This compound promotes lung autophagy and is valuable for research into Parkinson's disease and neuronopathic Gaucher disease, facilitating the study of its therapeutic potential in these conditions.
  23. Stable Isotope

    Omeprazole-13C,d3 is a stable isotope-labeled form of Omeprazole, a proton pump inhibitor (PPI) that targets gastric acid secretion. This compound is utilized in pharmacokinetic studies due to its competitive inhibition of CYP2C19 activity, with an inhibition constant (Ki) ranging from 2 to 6 μM. Additionally, Omeprazole exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria and acts as a potent inhibitor of neutral sphingomyelinase (N-SMase), impacting exosome release. It is a valuable reagent for research in gastrointestinal physiology, drug metabolism, and cellular signaling pathways.
  24. Stable Isotope

    Clarithromycin-d3 is a deuterium-labeled derivative of Clarithromycin, primarily used as a stable isotope. Clarithromycin exhibits a broad spectrum of antimicrobial activity and inhibits the CYP3A4-mediated alpha-hydroxylation of triazolam, showing an IC50 value of 56 μM. Additionally, it significantly affects hERG potassium currents and disrupts autophagic flux by interfering with the signaling pathway between hERG1 and PI3K. This reagent is valuable for research applications involving drug metabolism, ion channel activity, and cellular signaling pathways.
  25. Stable Isotope

    Felodipine-d3 is a deuterated form of Felodipine, a potent vasoselective calcium channel antagonist. It effectively lowers blood pressure by selectively targeting vascular smooth muscle, particularly in resistance vessels. In addition to its antihypertensive properties, Felodipine has been shown to induce autophagy and can penetrate the blood-brain barrier, making it useful for various biological studies and drug development research applications. This stable isotope is ideal for pharmacokinetic and metabolic studies involving Felodipine.
  26. Stable Isotope

    Theophylline-d6 is a deuterium-labeled analog of Theophylline, primarily utilized as a stable isotope in research. Theophylline functions as a nonselective phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist, while also acting as an activator of histone deacetylase (HDAC). This compound is valuable in studies exploring cellular signaling pathways, pharmacology, and the biochemical mechanisms underlying various therapeutic effects.
  27. Stable Isotope

    Ivacaftor-d18 is the deuterated form of Ivacaftor, a selective CFTR potentiator. It effectively targets G551D-CFTR and F508del-CFTR, demonstrating EC50 values of 100 nM and 25 nM, respectively. This stable isotope is essential for research applications related to cystic fibrosis, providing a tool for in vivo studies and pharmacokinetic analyses.
  28. Stable Isotope

    Glyburide-d11 is a deuterium-labeled analog of Glibenclamide, primarily acting as an ATP-sensitive K+ channel (KATP) inhibitor. It plays a crucial role in diabetes and obesity research by inhibiting P-glycoprotein and blocking the SUR1 subunits of KATP. Furthermore, Glyburide-d11 affects mitochondrial bioenergetics by altering membrane ion permeability and can induce autophagy, making it a valuable tool for studying cellular metabolism and drug response.
  29. Stable Isotope

    Homovanillic acid-d3 is a deuterium-labeled derivative of Homovanillic acid, serving as a stable isotope for research applications. This dopamine metabolite is implicated in various clinical conditions, including aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency. Homovanillic acid-d3 can be utilized in metabolic studies, investigations of neurotransmitter pathways, and the assessment of metabolic disorders.
  30. Stable Isotope

    Reserpine-d9 is a deuterated form of Reserpine that serves as an inhibitor of the vesicular monoamine transporter 2 (VMAT2). This stable isotope-labeled compound is valuable for studies in neuropharmacology and metabolism, allowing for precise tracking and quantification of Reserpine interactions in various biological systems. It enables researchers to explore its effects on neurotransmitter release and potential applications in psychiatric and neurological disorders.
  31. Stable Isotope

    Telmisartan-d3 is a deuterium-labeled derivative of Telmisartan, a potent and long-lasting antagonist of the angiotensin II type 1 receptor (AT1). This compound selectively inhibits the binding of 125I-AngII to AT1 receptors, exhibiting an IC50 value of 9.2 nM. Telmisartan-d3 serves as a valuable stable isotope for pharmacokinetic studies and in investigations involving the modulation of blood pressure and related cardiovascular research.
  32. Stable Isotope

    Pyrazinamide-d3 is a deuterium-labeled form of the antitubercular antibiotic pyrazinamide. This compound functions as a prodrug, which is metabolically converted to its active form, pyrazinoic acid (POA), by the enzyme nicotinamidase/PZase, encoded by the pncA gene in Mycobacterium tuberculosis. Pyrazinamide-d3 is utilized in metabolic studies and tracer experiments to investigate tuberculosis drug metabolism and efficacy. Its stable isotope labeling aids in the quantification and analysis of pyrazinamide’s pharmacokinetics in biological systems.
  33. Stable Isotope

    Ezetimibe-d4-1 is a deuterium-labeled derivative of Ezetimibe, a potent inhibitor of cholesterol absorption. Targeting the Niemann-Pick C1-like 1 (NPC1L1) protein, Ezetimibe effectively reduces intestinal cholesterol uptake. This compound is useful in research applications focused on lipid metabolism, cholesterol regulation, and the activation of Nrf2 pathways.
  34. Stable Isotope

    Oleanolic acid-d3 is a stable isotope-labeled form of oleanolic acid, a natural pentacyclic triterpenoid. Known for its anti-tumor properties, oleanolic acid has been widely studied for its potential therapeutic applications in various cancers. This compound serves as a valuable tool for researchers investigating metabolic pathways and pharmacokinetics in studies involving oleanolic acid.
  35. Stable Isotope

    Carbamazepine-d8 is a deuterium-labeled analogue of Carbamazepine, primarily targeting sodium channels. This stable isotope is utilized in pharmacokinetic studies and metabolic research to accurately trace drug metabolism and pharmacodynamics. The compound manifests anticonvulsant properties, contributing to its applications in epilepsy research and related neurological studies.
  36. Stable Isotope

    Ezetimibe-d4 is a stable isotope-labeled variant of Ezetimibe, a potent inhibitor of cholesterol absorption. By targeting the Niemann-Pick C1-like 1 (NPC1L1) protein, Ezetimibe-d4 effectively reduces intestinal cholesterol uptake, making it a valuable tool in lipid metabolism research. Additionally, this compound serves as an Nrf2 activator, highlighting its utility in studies related to oxidative stress and cellular defense mechanisms.
  37. Stable Isotope

    Fenofibrate-d6 is a deuterium-labeled version of Fenofibrate, a selective agonist of the peroxisome proliferator-activated receptor alpha (PPARα) with an EC50 value of 30 μM. This compound is also known to inhibit several human cytochrome P450 isoforms, exhibiting IC50 values of 0.2 μM for CYP2C19, 0.7 μM for CYP2B6, 9.7 μM for CYP2C9, 4.8 μM for CYP2C8, and 142.1 μM for CYP3A4. Fenofibrate-d6 is valuable for pharmacokinetic studies and metabolic research involving lipid modulation and drug metabolism.
  38. Stable Isotope

    Chenodeoxycholic acid-13C is the stable isotope version of Chenodeoxycholic Acid, a hydrophobic primary bile acid. This compound primarily activates the farnesoid X receptor (FXR), playing a crucial role in regulating cholesterol metabolism. Chenodeoxycholic acid-13C can be used in metabolic studies and tracer experiments, providing insights into bile acid physiology and its impacts on lipid homeostasis.
  39. Stable Isotope

    Apigenin-d5 is a deuterated analog of Apigenin, a flavonoid known for its ability to competitively inhibit CYP2C9 with a Ki of 2 μM. This stable isotope-labeled compound is suitable for use in pharmacokinetic studies and metabolic profiling, enabling precise quantification in biological samples. Its structural similarity allows for the investigation of Apigenin's biological effects and mechanisms of action in various research applications.
  40. Stable Isotope

    Meglutol-d3 is a deuterium-labeled analogue of Meglutol, a potent antilipemic agent. It effectively reduces cholesterol, triglycerides, serum beta-lipoproteins, and phospholipids by inhibiting hydroxymethylglutaryl-CoA reductase, the key enzyme in cholesterol biosynthesis. Meglutol-d3 is valuable in metabolic research and studies focusing on lipid metabolism and cardiovascular health.
  41. Stable Isotope

    Acetyl coenzyme A-d3 is a deuterium-labeled form of Acetyl coenzyme A, functioning as a stable isotope. This critical metabolic intermediate is involved in the TCA cycle and oxidative phosphorylation, playing a vital role in cellular energy production. Acetyl coenzyme A-d3 serves as the primary donor of acetyl groups for post-translational acetylation of proteins, influencing various cellular mechanisms. Additionally, it acts as a key precursor in lipid biosynthesis, making it valuable for metabolic and lipid research applications.
  42. Stable Isotope

    Trimetazidine-d8 dihydrochloride is a deuterium-labeled form of Trimetazidine, which selectively inhibits long-chain 3-ketoyl coenzyme A thiolase with an IC50 of 75 nM, effectively blocking β-oxidation of free fatty acids. It functions as an antianginal and cytoprotective agent, exhibiting antioxidant, anti-inflammatory, antinociceptive, and gastroprotective properties. Additionally, Trimetazidine-d8 dihydrochloride activates autophagy and inhibits 3-hydroxyacyl-CoA dehydrogenase (HADHA), making it a crucial tool for research into cellular metabolism and cardiac function.
  43. Stable Isotope

    Letrozole-d4 is a deuterium-labeled analogue of Letrozole, a selective non-steroidal aromatase inhibitor. It effectively inhibits estrogen biosynthesis with an IC50 of 11.5 nM, making it a valuable tool for studying the mechanisms of estrogen-dependent tumor growth in breast cancer research. This stable isotopic variant facilitates advanced metabolic studies and pharmacokinetic analyses in various experimental settings.
  44. Stable Isotope

    Retinoic acid-d6 is a deuterium-labeled derivative of retinoic acid, a crucial metabolite of vitamin A. It functions primarily as an agonist of retinoic acid receptors (RAR), exhibiting IC50 values of 14 nM for RARα, RARβ, and RARγ. Additionally, retinoic acid-d6 binds to PPARβ/δ with a Kd of 17 nM and inhibits the transcription factor Nrf2 through the activation of retinoic acid receptor alpha. This compound is valuable for studies involving cellular growth, differentiation, and organogenesis, as well as for investigating the regulatory mechanisms of nuclear receptors in research applications.
  45. Stable Isotope

    Sertindole-d4 is a deuterium-labeled analog of Sertindole, a second-generation antipsychotic agent. The incorporation of deuterium enhances the stability and specificity of metabolic studies involving Sertindole. This stable isotope is useful for pharmacokinetic and pharmacodynamic research, allowing for detailed investigations into the drug's metabolism and behavior in biological systems.
  46. Stable Isotope

    Tizoxanide-d4 is a deuterated form of Tizoxanide, serving as a stable isotope for research applications. Tizoxanide is the bioactive metabolite of Nitazoxanide, demonstrating potent anti-infective properties against anaerobic bacteria, protozoa, and various viruses, including HIV-1. This compound is essential for studies involving metabolic pathways, pharmacokinetics, and the development of antiviral therapies.
  47. Stable Isotope

    Desmethyl Naproxen-d3 is a deuterium-labeled derivative of Desmethyl Naproxen, a primary metabolite of the anti-inflammatory drug Naproxen. This stable isotope is utilized in pharmacokinetic studies to track and quantify the metabolism and distribution of Naproxen in biological systems. It plays a significant role in elucidating drug interactions and optimizing therapeutic strategies in inflammation research.
  48. Stable Isotope

    Amiodarone-d4 hydrochloride is a deuterium-labeled derivative of the Class III antiarrhythmic agent, Amiodarone hydrochloride, which primarily targets the human ether-a-go-go-related gene (hERG) potassium channel with an IC50 of approximately 45 nM. This compound influences vital cellular processes, promoting fibroblast proliferation and myofibroblast differentiation through the activation of ERK1/2 and p38 MAPK signaling pathways. Amiodarone-d4 hydrochloride is an essential tool for research into supraventricular and ventricular arrhythmias, providing valuable insights into arrhythmia mechanisms and potential therapeutic strategies.
  49. Stable Isotope

    Topotecan-d6 is a deuterated form of Topotecan, a potent inhibitor of Topoisomerase I, which plays a critical role in DNA replication and repair. This compound exhibits significant biological activity, with IC50 values of approximately 2.73 μM in U251 cells, 2.95 μM in U87 cells, and ranging from 5.46 to 5.95 μM in glioblastoma stem cells (GSCs-U251 and GSCs-U87). Topotecan-d6 is ideal for studies involving drug metabolism, pharmacokinetics, and cancer research, particularly in understanding the mechanisms of action of Topoisomerase I inhibitors.
  50. Stable Isotope

    Memantine-d6 hydrochloride is a deuterium-labeled analog of Memantine hydrochloride, functioning primarily as a stable isotope in research. Memantine acts as an uncompetitive antagonist of the NMDA receptor, exhibiting moderate affinity, and also inhibits the cytochrome P450 enzymes CYP2B6 and CYP2D6 with inhibition constants of 0.51 nM and 94.9 μM, respectively. This compound is invaluable for studies involving neuropharmacology, metabolic profiling, and isotope labeling in drug development and mechanistic investigations.

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