Isotope-Labeled Compounds

Clarithromycin-13C,d3 is a stable isotope-labeled form of the macrolide antibiotic Clarithromycin, incorporating deuterium and carbon-13 isotopes. This compound serves as a valuable tool in pharmacokinetic studies, enabling the tracing of metabolic pathways and the investigation of drug interactions. Its precise labeling facilitates quantitative analysis in biological and clinical research, enhancing the understanding of Clarithromycin's pharmacodynamics and bioavailability.

Irinotecan-d10 hydrochloride is a deuterium-labeled derivative of Irinotecan, a potent inhibitor of topoisomerase I. It functions by binding to the topoisomerase I-DNA complex, thereby preventing the religation of DNA strands and disrupting DNA replication. This reagent is widely used in pharmacokinetic studies, drug metabolism research, and the development of therapeutic strategies targeting topoisomerase I.

Niacin-13C6 is a stable isotope-labeled form of Niacin (Nicotinic acid), a key vitamin in the B group. This compound serves as an essential dietary nutrient and plays a vital role in various metabolic processes, including the conversion of nutrients into energy. Niacin-13C6 is predominantly used in metabolic studies and tracer experiments to investigate vitamin B metabolism and its effects on physiological functions.

Iohexol-d5 is a deuterated form of Iohexol, serving as a stable isotope for analytical applications. As a radiographic contrast agent, Iohexol is utilized in various imaging techniques, including myelography, computerized tomography, cisternography, and ventriculography. This compound is valuable in enhancing imaging clarity and sensitivity in in vivo studies, making it essential for diagnostic imaging research.

4-Hydroxytolbutamide-d9 is a deuterium-labeled derivative of 4-Hydroxytolbutamide, a metabolite of the oral antidiabetic agent Tolbutamide. This compound primarily targets cytochrome P450 enzymes CYP2C8 and CYP2C9, which are involved in its metabolism. It is utilized in pharmacokinetic studies and metabolic profiling to trace the metabolic pathways of sulfonylureas and to assess their efficacy in diabetes research.

Isoniazid-d4 is a deuterium-labeled derivative of Isoniazid, a prodrug requiring activation by the bacterial catalase-peroxidase enzyme KatG. It exhibits bactericidal activity against rapidly dividing mycobacteria, making it a critical agent in the treatment of tuberculosis. This stable isotope can be utilized in pharmacokinetic studies and tracing experiments to elucidate metabolic pathways and drug interactions within clinical and research settings.

Cabazitaxel-d9 is a deuterated derivative of Cabazitaxel, a semi-synthetic analog of the natural taxoid 10-deacetylbaccatin III. This compound exhibits potential antineoplastic activity by stabilizing microtubules and inhibiting cancer cell division. Cabazitaxel-d9 serves as a valuable stable isotope for in vivo and in vitro studies, facilitating the investigation of pharmacokinetics and the mechanistic action of Cabazitaxel in cancer research.

Enoxacin-d8 hydrochloride is a deuterium-labeled derivative of enoxacin, which primarily targets bacterial DNA gyrase and topoisomerase IV, exhibiting inhibitory activities with IC50 values of 126 µg/ml and 26.5 µg/ml, respectively. It functions as a miRNA processing activator, enhancing siRNA-mediated mRNA degradation and promoting the biogenesis of endogenous miRNAs. Additionally, enoxacin exhibits significant antibacterial properties against both gram-positive and gram-negative organisms and serves as a cancer-specific growth inhibitor by facilitating microRNA processing via TAR RNA-binding protein 2 (TRBP). This compound is valuable for applications requiring stable isotopes in biochemical and pharmacological research.

N-Dodecyl-β-D-maltoside-d25 is a deuterium-labeled non-ionic detergent that serves as a stable isotope. This compound exhibits strong adsorption properties on materials such as alumina, titanium dioxide, and hematite. N-Dodecyl-β-D-maltoside-d25 is effective in promoting the reactivation of various proteins and stabilizing photoactive reaction center complexes, particularly inhibiting the degradation of Rhodopseudomonas spheroides R-26 reaction centers in solution. Its applications include the purification and stabilization of RNA polymerase, as well as the investigation of protein-lipid interactions.

Folic acid-d2 is a stable isotope-labeled form of folic acid (Vitamin B9), crucial for nucleotide synthesis and cellular proliferation. As a B vitamin, it plays a vital role in DNA and RNA synthesis, supporting essential cellular functions. This reagent is applicable in metabolic studies, tracer experiments, and research involving folate metabolism and its physiological implications.

TK216-d4 is a deuterated analog of TK216, a potent E26 transformation specific (ETS) inhibitor. It functions by directly binding to the EWS-FLI1 fusion protein, inhibiting its interactions with critical partners such as RNA helicase A. This compound is primarily used in cancer research, particularly in studies focused on the mechanisms of ETS-driven tumors and the cellular pathways influenced by EWS-FLI1. Its stable isotope labeling allows for precise tracking and analysis in biological systems.

Deoxythymidine-5'-triphosphate-d15 dilithium is a deuterium-labeled analog of deoxythymidine-5'-triphosphate (dTTP), serving as a stable isotope. As a key nucleoside triphosphate, dTTP plays a critical role in DNA synthesis, facilitating incorporation into growing DNA strands during replication. This reagent is particularly useful in studies involving nucleic acid metabolism and dynamics, enabling researchers to track and quantify DNA synthesis processes in vitro and in vivo.

Thymine-13C is a stable isotope-labeled form of thymine, one of the four essential nucleobases in DNA. This compound serves as a valuable tool in the study of nucleic acid metabolism and cancer research, particularly in evaluating the interaction of thymine with chemotherapeutic agents such as 5-fluorouracil (5-FU), which has a Km of 2.3 μM. Thymine-13C can facilitate advanced techniques such as tracer studies and metabolic profiling, enhancing the understanding of biochemical pathways in various cellular contexts.

GS-441524-d is a deuterium-labeled analog of GS-441524, a key metabolite of Remdesivir. It exhibits notable antiviral efficacy against various coronaviruses, demonstrating comparable effectiveness in cell-based models involving primary human lung and cat cells. Additionally, GS-441524 effectively inhibits feline infectious peritonitis virus (FIPV) with an EC50 value of 0.78 μM, making it a valuable reagent for research on coronavirus-related infections and treatments.

3'-Deoxy-3'-fluorothymidine-d3 is a deuterium-labeled derivative of Alovudine, primarily targeting mitochondrial DNA synthesis inhibition. This compound serves as a specific marker for DNA synthesis and demonstrates reduced susceptibility to inflammatory changes compared to conventional markers, making it particularly useful in pancreatic cancer research. Additionally, Alovudine exhibits anti-orthopoxvirus and anti-leukemic properties, further broadening its applicability in studying viral infections and hematological malignancies.

2'-Deoxyadenosine-5'-triphosphate-d14 dilithium is a deuterium-labeled form of 2'-deoxyadenosine-5'-triphosphate (dATP). This nucleotide serves as a critical substrate in cellular DNA synthesis and replication, functioning as an essential component for DNA polymerase activity. Its stable isotope labeling allows for advanced applications in metabolic tracing and mechanistic studies in molecular biology.

Pseudouridine-13C,15N2 is a stable isotope-labeled derivative of pseudouridine. As an isomer of uridine, pseudouridine plays a critical role in the modification of non-coding RNA and is the most abundant modified nucleoside in these molecules. It enhances the stability and function of rRNA and tRNA, which are essential for accurate mRNA decoding and translation processes. Pseudouridine-modified tRNA fragments are also significant in studies related to myelodysplastic syndrome (MDS)-associated leukemias, offering potential insights into aberrant protein synthesis mechanisms.

Thymidine-2′-13C is a stable isotope-labeled form of thymidine, specifically incorporating carbon-13 at the 2' position. This compound functions as a key precursor in the synthesis of deoxyribonucleic acid (DNA) and can act as a cell synchronizing agent, effectively arresting cells at the G1/S boundary prior to DNA replication. Thymidine-2′-13C is valuable in metabolic studies, tracer experiments, and investigations related to DNA metabolism and cell cycle regulation.

N-Nitrosodibenzylamine-d10 is a deuterated form of N-Nitrosodibenzylamine, functioning as a stable isotope. This compound is recognized for its ability to induce DNA damage, specifically by promoting DNA single-strand breaks (SSBs). N-Nitrosodibenzylamine-d10 is utilized in research applications focusing on DNA damage mechanisms and the study of mutagenic processes.

rU Phosphoramidite-15N is a stable isotope-labeled monomer specifically designed for the synthesis of oligonucleotides. This phosphoramidite incorporates nitrogen-15 labeling, enhancing the study and analysis of RNA structures and interactions. Its applications extend to nucleic acid research, including studies on RNA stability, folding, and binding kinetics.

Folic acid-13C5,15N is a stable isotope-labeled form of folic acid, incorporating five carbon-13 and one nitrogen-15 atoms. This compound serves as a valuable tracer for metabolic studies, specifically in the investigation of folate metabolism and associated biological pathways. It is suitable for applications in pharmacokinetic studies, nutrition research, and isotope labeling experiments to enhance the understanding of folate-related processes in various biological systems.

Ac-rC Phosphoramidite-15N is a stable isotope-labeled derivative of Ac-rC Phosphoramidite, incorporating nitrogen-15 in its structure. This reagent is utilized for the synthesis of oligoribonucleotides with phosphorodithioate modifications (PS2-RNA), which are important for enhancing the stability and biological activity of RNA molecules. Its application in chemical research facilitates studies in RNA function and interactions, enabling the exploration of therapeutic strategies targeting RNA-based pathways.

Levomefolic acid-13C5 is a stable isotope-labeled form of Levomefolic acid (L-5-MTHF), which serves as a bioactive compound in the folate pathway. This naturally occurring derivative of folic acid is known for its ability to cross the blood-brain barrier and is utilized in various nutritional studies and research applications. Levomefolic acid-13C5 is particularly useful in metabolic tracing and pharmacokinetic studies involving folate metabolism.

Deoxythymidine-5'-triphosphate-13C10,15N2 dilithium is a stable isotope-labeled form of deoxythymidine-5'-triphosphate (dTTP), incorporating both carbon-13 and nitrogen-15 isotopes. As one of the four nucleoside triphosphates, dTTP plays a crucial role in DNA synthesis, serving as a substrate for DNA polymerases. This reagent is essential for advanced biochemical studies, including metabolic tracing, DNA sequencing, and mechanistic investigations in nucleic acid research.

Butylparaben-d9 is a stable isotope-labeled form of Butyl parahydroxybenzoate, designated for use in quantitative analyses and research applications. This deuterium-labeled compound serves as a useful internal standard in mass spectrometry techniques, helping to improve the accuracy of quantification of Butylparaben in various matrices. Its incorporation into research on pharmacokinetics and toxicology contributes to a deeper understanding of paraben-related studies.

N-Nitrosodiethylamine-d4 is a deuterated form of the potent hepatocarcinogen N-Nitrosodiethylamine (DEN), which functions as a dialkylnitrosoamine. This compound is primarily found in various sources, including tobacco smoke, certain foods, and alcoholic beverages, and is known to induce significant alterations in nuclear enzymes related to DNA repair and replication. Research demonstrates that N-Nitrosodiethylamine can lead to tumor formation across multiple animal species, particularly affecting the nasal cavity, trachea, lungs, esophagus, and liver. This stable isotope is valuable for studies involving metabolic pathways and the mechanisms of carcinogenesis.

Docosanoic acid-13C4, a stable isotope-labeled form of docosanoic acid (behenic acid), primarily targets the p53 DNA binding domain, inhibiting its double-stranded DNA binding activity with a Kd of 12 nM. This long-chain saturated fatty acid is utilized in research applications to study lipid metabolism and the regulation of cholesterol levels. Given its low bioavailability, docosanoic acid-13C4 serves as a valuable tool for investigating the implications of fatty acid interactions within biological systems.

Thymidine-d2 is a stable isotope-labeled form of thymidine, serving as a crucial precursor in deoxyribonucleic acid synthesis. This compound operates primarily by inhibiting DNA synthesis, effectively arresting cell cycle progression at the G1/S boundary, which is pivotal in studies of cell synchrony and replication dynamics. Thymidine-d2 is valuable in metabolic labeling experiments and tracing DNA synthesis pathways in various biological research applications.

Guanine-13C2,7-15N is a stable isotope-labeled form of guanine, incorporating both carbon-13 and nitrogen-15 isotopes. As a crucial component of nucleic acids, guanine plays significant roles in cellular metabolism and genetic information processing. Its unique labeling allows for enhanced tracking and analysis in metabolic studies, as well as investigations into nucleic acid structure and function. Additionally, guanine exhibits cytotoxic, antinociceptive, and neuroprotective properties, making it valuable for research in neurobiology and pharmacology.

2-Aminofluorene-d11 is a deuterated derivative of 2-Aminofluorene, which acts as a genotoxin. This stable isotope is valuable for studying DNA adduct formation, mechanisms of DNA repair, and processes related to carcinogenesis and mutagenesis. Its unique labeling facilitates advanced research in environmental and toxicological studies, providing insights into the effects of genotoxic agents on biological systems.

Docosanoic acid-d4-2 is a deuterium-labeled derivative of Docosanoic acid, a long-chain saturated fatty acid. This compound primarily functions as a stable isotope, suitable for tracing studies in biological research. Docosanoic acid exhibits the ability to inhibit the double-stranded DNA binding activity of the p53 DNA binding domain, showing a binding affinity with a Kd of 12 nM. It may be useful in studies exploring lipid metabolism and p53-related pathways in human health and disease.

Guanine-13C2,15N is a stable isotope-labeled form of guanine, incorporating both 13C and 15N isotopes. As a critical component of nucleic acids (DNA and RNA), guanine is essential for various biological processes. This labeled compound can be utilized in metabolic studies, isotopic tracing experiments, and investigations into nucleic acid dynamics. Additionally, guanine exhibits cytotoxic, antinociceptive, and neuroprotective properties, making it a valuable tool in cellular and neurobiological research.

Oxolinic acid-d5 is a deuterium-labeled derivative of Oxolinic acid, primarily targeting bacterial RNA and DNA synthesis. This compound exhibits antibacterial activity against both Gram-negative and Gram-positive bacteria, making it valuable in studies addressing urinary tract infections. Additionally, Oxolinic acid has been shown to inhibit dopamine uptake and produce locomotor effects in murine models, facilitating research into neurological pathways and bacterial resistance mechanisms.

2-Aminofluorene-13C is the stable isotope-labeled derivative of 2-Aminofluorene, a synthetic chemical known for its genotoxic properties. This reagent is critical for investigating DNA adduct formation, elucidating mechanisms of DNA repair, and studying pathways of carcinogenesis and mutagenesis. It serves as a valuable tool in toxicology and cancer research, enabling detailed analysis of DNA interactions and their biological consequences.

Spermine-15N2 is a stable isotope-labeled form of Spermine, a natural polyamine that functions as an antioxidant and anti-inflammatory agent. This compound has been shown to inhibit certain bacterial cultures, particularly strains of Staphylococcus aureus, and induces neurotoxicity in a dose-dependent manner within the striatum. Spermine-15N2 also reversibly inhibits DNA synthesis and various immune responses in primary murine spleen cell cultures. Additionally, it acts as a nitric oxide donor, modulating platelet activation and demonstrating bioactive properties across different biological systems.

Thymidine-13C-1 is a stable isotope-labeled variant of thymidine, a key precursor in deoxyribonucleic acid synthesis. It effectively serves as a cell synchronizing agent, inhibiting DNA synthesis and arresting cells at the G1/S boundary before DNA replication occurs. This compound is widely used in cellular and molecular biology research to study DNA replication dynamics and cellular proliferation.

1,2-Dihydropyridazine-3,6-dione-3,4,5,6-13C4 is a stable isotope-labeled variant of maleic hydrazide, a known systemic plant growth regulator and herbicide. This compound functions primarily by inhibiting the synthesis of nucleic acids and proteins, thereby affecting plant growth and development. Its isotopic labeling allows for enhanced traceability in biochemical studies and plant metabolism research, making it a valuable tool in agricultural and environmental studies.

Cytidine-5'-triphosphate-13C5 is a stable isotope-labeled form of Cytidine-5'-triphosphate (5'-CTP), a crucial nucleoside triphosphate. It acts as a key building block for the synthesis of nucleotides and nucleic acids, as well as for lipid biosynthesis. The compound is primarily utilized in research applications involving the study of de novo pyrimidine biosynthesis and can aid in tracing metabolic pathways in various biological systems, including Toxoplasma gondii.

Deoxycytidine triphosphate-d14 dilithium is a deuterium-labeled form of deoxycytidine triphosphate (dCTP), specifically designed for stable isotope applications in molecular biology. This nucleoside triphosphate serves as a crucial substrate for DNA synthesis and is widely utilized in techniques such as real-time PCR, cDNA synthesis, and DNA sequencing. The incorporation of deuterium enhances the tracking and quantification of nucleic acids in various biochemical assays.

2,5-Deoxyfructosazine-13C4 is a stable isotope-labeled compound derived from 2,5-Deoxyfructosazine, known for its role as a flavoring agent in the food and tobacco industries. As a pyrazine derivative, it participates in biochemical research related to its DNA strand breakage activity and its ability to inhibit IL-2 production in Jurkat cells upon stimulation with phytohemagglutinin, with an IC50 of approximately 1.25 mM. 2,5-Deoxyfructosazine-13C4 serves as a valuable tool for tracing and understanding metabolic pathways and interactions involving pyrazine compounds.

Danofloxacin-d3 is a deuterium-labeled derivative of Danofloxacin, a potent orally active quinolone antibiotic. It primarily targets bacterial DNA gyrase, effectively inhibiting DNA replication, transcription, and bacterial growth. This reagent is valuable for research involving the study of bacterial infections caused by pathogens such as Escherichia coli and Mycoplasma, enabling detailed investigations of antibiotic mechanisms and efficacy.

Pazufloxacin-d4 is a deuterated derivative of the fluoroquinolone antimicrobial agent Pazufloxacin. This compound specifically targets DNA gyrase, demonstrating inhibitory activity with IC50 values of 0.88 μg/mL against E. coli and 1.9 μg/mL against P. aeruginosa. Pazufloxacin-d4 showcases broad-spectrum antimicrobial efficacy, with MIC90 values ranging between 0.025 to 100 μg/mL against various Gram-positive and Gram-negative bacteria, including non-fermenting pathogens and anaerobes. This reagent is suitable for investigating systemic and lung infections, as well as urinary tract infections and Legionella pneumonia in research contexts.

dGTP-155 (2'-Deoxyguanosine-5'-triphosphate-155) is a stable isotope-labeled nucleotide specifically designed for use in biochemical and molecular biology research. As a key component in deoxyribonucleic acid (DNA) synthesis, dGTP-155 plays a crucial role in the incorporation of guanine into nucleic acid strands. This compound is particularly important in studies investigating oxidative damage and the mechanisms of nucleotide metabolism, providing insights into guanosine nucleotide behavior under various biological conditions.

Pefloxacin-d3 is a deuterated derivative of the broad-spectrum antibiotic Pefloxacin, designed for stable isotope research applications. It primarily targets DNA gyrase, inhibiting DNA replication, and shows effective activity against various bacterial strains including Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis, with MIC90 values of 0.12, 4, and 16 mg/L, respectively. Additionally, Pefloxacin exhibits anti-Plasmodium yoelii activity and can enhance UVA-induced edema and immunosuppression. This reagent is suitable for infection studies and advanced biochemical assays.

Thymidine-d14 is a stable isotope-labeled analogue of thymidine, primarily utilized in DNA synthesis studies. As a specific precursor for deoxyribonucleic acid, it serves as an effective cell synchronizing agent by inhibiting DNA replication and arresting cells at the G1/S transition phase. This reagent is valuable for research applications involving cellular proliferation, DNA metabolism, and molecular labeling techniques.

DMT-dG(ib) Phosphoramidite-13C10,15N5 is a stable isotope-labeled phosphoramidite monomer featuring 13C and 15N isotopes. Its primary mechanism involves incorporation into oligonucleotide sequences, facilitating the synthesis of labeled DNA and related nucleic acids. This reagent is ideal for applications in nucleic acid research, including studies on DNA structure, function, and hybridization dynamics, as well as applications in biophysical and biochemical analyses.

Danofloxacin-d3-1 is a deuterium-labeled derivative of Danofloxacin, which is an orally active quinolone antibiotic. This compound primarily targets bacterial DNA gyrase, disrupting bacterial DNA replication, transcription, and overall growth. It is instrumental in the study of bacterial infections caused by pathogens such as Escherichia coli and Mycoplasma, providing valuable insights into antibiotic efficacy and resistance mechanisms.

Gimeracil-13C3 is a stable isotope-labeled form of Gimeracil, designed to facilitate advanced metabolic studies. As a key component of the oral fluoropyrimidine derivative S-1, Gimeracil inhibits DNA double-strand break repair and acts as a potent inhibitor of dihydropyrimidine dehydrogenase (DPD). This reagent can be utilized in research applications related to cancer therapeutics and molecular pharmacology, providing insights into the metabolic pathways of fluoropyrimidines.

Pefloxacin-d5 is a deuterated derivative of Pefloxacin, functioning primarily as a stable isotope for various research applications. This broad-spectrum antibiotic acts by inhibiting DNA gyrase, subsequently blocking DNA replication. Pefloxacin demonstrates antibacterial efficacy against pathogens such as Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis, with respective MIC90s of 0.12, 4, and 16 mg/L. Additionally, it exhibits activity against Plasmodium yoelii and may enhance UVA-induced edema and immunosuppression, rendering it valuable for infection and pharmacological studies.

N-Nitrosodibenzylamine-d4 is a deuterium-labeled analog of N-Nitrosodibenzylamine, primarily used as a stable isotope in biological research. This compound acts as a potent DNA damage inducer, specifically inducing DNA single-strand breaks (SSBs). Its applications include studies on genotoxicity, DNA repair mechanisms, and the investigation of cellular responses to DNA damage.