Isotope-Labeled Compounds

Azilsartan-d4 is a deuterium-labeled analog of Azilsartan, a potent and selective antagonist of the angiotensin II type 1 receptor (AT1). This stable isotope plays a key role in tracing and quantifying the pharmacokinetics of Azilsartan in biological systems. Additionally, Azilsartan promotes reactive oxygen species (ROS) formation and apoptosis in HepG2 cancer cells, demonstrating potential neuroprotective and anticancer properties. It is applicable in research focused on hypertension and stroke mechanisms.

Adenosine-d-1 is a deuterium-labeled derivative of adenosine, an endogenous autacoid that interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3. This stable isotope serves as a valuable tool for studying adenosine's diverse biological functions and its role in various physiological and pathological processes. Applications include pharmacological research, metabolic studies, and the investigation of signal transduction pathways mediated by adenosine receptors.

Glyphosate-13C,15N-1 is a stable isotope-labeled version of Glyphosate, a non-selective systemic herbicide targeting the 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) in the shikimic acid pathway. This inhibition disrupts the biosynthesis of crucial aromatic amino acids, including tyrosine, phenylalanine, and tryptophan. Glyphosate-13C,15N-1 is valuable in research applications focused on elucidating herbicide metabolism, environmental monitoring, and studying its impact on oxidative stress, neuroinflammation, and mitochondrial dysfunction that can lead to neuronal death and associated behavioral disorders.

Oxaliplatin-d10 is a deuterium-labeled derivative of Oxaliplatin, an effective DNA synthesis inhibitor. Its primary mechanism involves the induction of DNA crosslinking, which disrupts DNA replication and transcription, ultimately leading to apoptosis in cancer cells. This stable isotope is valuable for cancer research, particularly in studies focused on drug metabolism and pharmacokinetics.

Amiloride-15N3 hydrochloride is a stable isotope-labeled form of Amiloride hydrochloride, primarily targeting the epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). This compound functions as an inhibitor, blocking ENaC and PC2 (TRPP2) channels, making it a valuable tool in research applications related to sodium transport and renal physiology. It is particularly useful in studies requiring isotopically enriched compounds for elucidating metabolic pathways or pharmacokinetics.

Pantoprazole-d3 is a deuterium-labeled form of Pantoprazole, a potent proton pump inhibitor (PPI) that selectively targets the H+/K+-ATPase enzyme, exhibiting an IC50 of 6.8 μM. This compound enhances gastric pH stability and demonstrates significant anti-secretory and anti-ulcer properties. It is utilized in research to study gastric acid secretion mechanisms and to investigate potential synergistic effects with chemotherapeutic agents, such as Doxorubicin, in cancer treatment.

Bendamustine-d8 hydrochloride is a deuterium-labeled analog of Bendamustine hydrochloride, targeting DNA as a cross-linking agent. This reagent facilitates the activation of DNA-damage stress response pathways and triggers apoptosis. With its potent alkylating and anticancer properties, Bendamustine-d8 hydrochloride is valuable for research applications involving cancer biology, drug metabolism studies, and molecular mechanisms of chemotherapeutic agents.

Isobutylparaben-d4 is a deuterated derivative of Isobutylparaben, functioning as a stable isotope for analytical studies. Isobutylparaben is recognized for its agonistic activity on the nuclear receptors PXR, CAR, and PPAR. Its antimicrobial properties make it valuable in various research contexts, particularly in evaluating safety and efficacy in personal care products and cosmetics. This reagent is essential for studies requiring isotopic labeling for mass spectrometry or related techniques.

(±)-Enterodiol-13C3 is a stable isotope-labeled derivative of (±)-Enterodiol, which is derived from lignans present in whole grains, nuts, legumes, flaxseed, and vegetables through microbial metabolism in the human intestine. This compound exhibits significant apoptotic effects in colorectal cancer cells and demonstrates anti-cancer activities. (±)-Enterodiol-13C3 is valuable for metabolic studies and investigations into the mechanisms of cancer biology, enabling researchers to trace metabolic pathways and interactions in biological systems.

Higenamine-d4 hydrochloride is a deuterium-labeled form of Higenamine, acting as a stable isotope. It is utilized in chemical research for studies involving pharmacokinetics, metabolic tracing, and isotopic labeling in biological systems. This reagent aids in the development and validation of analytical methods, enhancing the accuracy of quantitative assessments in various biological applications.

Azoxystrobin-d4 is a deuterium-labeled derivative of Azoxystrobin, a broad-spectrum β-methoxyacrylate fungicide. It primarily targets the Qo site of the cytochrome bc1 complex, inhibiting mitochondrial respiration and electron transfer. This compound is known to induce the production of reactive oxygen species (ROS), leading to cellular apoptosis. Azoxystrobin-d4 is utilized in research applications focused on mitochondrial function and fungal pathogenesis.

L-Ascorbic acid-13C-4 is a stable isotope-labeled form of L-Ascorbic acid, an endogenous antioxidant and electron donor. This compound exhibits selective inhibition of Cav3.2 channels with an IC50 of 6.5 μM. It is commonly utilized in research applications studying cellular processes, oxidative stress, and collagen synthesis.

Vandetanib-d6 is a deuterium-labeled derivative of Vandetanib, a potent and orally active inhibitor of the VEGFR2/KDR tyrosine kinase with an IC50 value of 40 nM. This compound also exhibits inhibition against VEGFR3/FLT4 (IC50 = 110 nM) and EGFR/HER1 (IC50 = 500 nM). Vandetanib-d6 is particularly valuable in pharmacokinetic studies and metabolic research involving Vandetanib, as it enables the tracking of the compound's bioavailability and distribution in vivo.

Tilmicosin-d3 is a deuterium-labeled derivative of Tilmicosin, which acts primarily as a calcium channel antagonist and macrolide antibiotic. It targets the 50S subunit of bacterial ribosomes, effectively inhibiting protein synthesis and exhibiting significant antimicrobial activity. Tilmicosin is particularly useful for addressing respiratory diseases in livestock, including cattle, sheep, and pigs. Additionally, it possesses immunomodulatory and anti-inflammatory properties, making it valuable for various research applications in veterinary medicine and pharmacology.

L-Asparagine-4-13C monohydrate is a stable isotope-labeled form of the amino acid L-Asparagine. This compound serves as an essential substrate for L-Asparaginase, an enzyme utilized in the treatment of leukemia due to its ability to deplete asparagine, thereby inhibiting RNA and DNA synthesis in lymphoblasts and inducing apoptosis. L-Asparagine-4-13C monohydrate is valuable in research applications, including its use as a biomarker for investigating childhood acute lymphoblastic leukemia and studying metabolic pathways in cancer cells with low asparagine synthetase expression.

Carbaryl-d3 is a deuterium-labeled variant of Carbaryl, characterized as an acetylcholinesterase inhibitor. This compound prevents the breakdown of acetylcholine in the synaptic cleft, resulting in its accumulation and subsequent neurotoxic effects. Carbaryl-d3 is employed in research related to neurotoxicity mechanisms and may serve as a tool for studying the pharmacokinetics and metabolic pathways of Carbaryl. Its stable isotope labeling enhances analytical precision in experimental applications.

Picropodophyllin-d3 is a deuterium-labeled derivative of Picropodophyllin, specifically characterized as an insulin-like growth factor-1 receptor (IGF-1R) inhibitor, exhibiting an IC50 of 1 nM. This stable isotope is designed for use in metabolic studies and tracer experiments, providing enhanced sensitivity and precision in research applications. Its selective inhibition of IGF-1R makes it a valuable tool for investigating signaling pathways involved in cancer and metabolic disorders.

Formamide-15N is a stable isotope-labeled formamide, featuring nitrogen-15 (15N). It serves as an effective DNA denaturant, significantly destabilizing DNA structure in buffer systems, which is crucial for various molecular biology applications. In addition, formamide acts as a decalcifying agent for cardiac cells and is commonly utilized as a solvent or raw material in the synthesis of ion compounds, resins, and plasticizers, making it versatile for chemical research.

Irbesartan-d6-1 is a deuterated form of Irbesartan, a well-studied antagonist of the Ang II type 1 (AT1) receptor. This compound effectively promotes vasodilation, leading to reduced blood pressure and enhanced myocardial oxygenation. Irbesartan-d6-1 is valuable for research focused on hypertension, heart failure, and diabetic nephropathy, providing insights into the pharmacodynamics and pharmacokinetics of its parent compound in various biological systems.

Sodium butyrate-d5 is a deuterated derivative of sodium butyrate, serving as a stable isotope for research applications. It functions primarily as a histone deacetylase (HDAC) inhibitor, demonstrating notable anti-tumor activity. This reagent is useful for studies on gene expression, epigenetic regulation, and cancer biology, facilitating the investigation of the mechanisms underlying cellular processes and therapeutic responses.

Ketoprofen-d4 is the deuterated form of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that primarily acts as a potent inhibitor of cyclooxygenase (COX) enzymes. It demonstrates significant inhibitory activity with IC50 values of 2 nM for COX-1 and 26 nM for COX-2 in human blood monocytes. Ketoprofen-d4 is used in chemical research to study the metabolism and pharmacokinetics of Ketoprofen, helping to elucidate its biological effects and therapeutic applications.

Formamide-d2 is a deuterated isotope of formamide, functioning primarily as a stable isotope in chemical research. It serves as an effective DNA denaturant, significantly destabilizing DNA structures in buffer solutions, which is crucial for various molecular biology applications. Furthermore, formamide-d2 can be utilized as a decalcifying agent in rat cardiac cells and is commonly employed as a solvent for ion compounds, resins, and plasticizers in synthetic chemistry.

Panobinostat-d4 is a deuterium-labeled derivative of Panobinostat, a potent non-selective histone deacetylase (HDAC) inhibitor with significant antineoplastic properties. This compound effectively induces HIV-1 production in latently infected cells at low concentrations, enhancing viral expression and facilitating studies on HIV latency. Additionally, Panobinostat promotes apoptosis and autophagy in cancer cells, making it valuable for research on refractory or relapsed multiple myeloma.

D-Mannitol-d2 is a deuterium-labeled derivative of D-Mannitol, primarily used as a stable isotope in various research applications. D-Mannitol is an osmotic diuretic with significant biological activity, promoting calcium and magnesium absorption while reducing tissue edema. Additionally, it has been shown to enhance brown adipocyte formation and improve insulin sensitivity by activating the β3-adrenergic receptor pathway, leading to the conversion of white fat cells into brown fat. This compound is particularly useful in studies involving osmotic pressure regulation and cellular protection in plant and mammalian cell cultures.

Ibuprofen-13C,d3 is a stable isotope-labeled form of Ibuprofen, incorporating both carbon-13 and deuterium. This compound functions as a nonsteroidal anti-inflammatory drug, primarily targeting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), with reported IC50 values of 13 μM and 370 μM, respectively. It serves as a valuable tool in metabolic tracing studies and in investigations of pharmacokinetics and drug metabolism.

Olanzapine-d8 is a deuterated derivative of Olanzapine, primarily functioning as a stable isotope for research applications. As an atypical antipsychotic, Olanzapine exhibits high-affinity binding to multiple receptors including serotonin (H1, 5HT2A/2C, 5HT3, 5HT6), dopamine (D1-4), and muscarinic receptors, as well as adrenergic α1 receptors. This compound is valuable in pharmacological studies focused on the mechanisms of antipsychotic activity and the profiling of monoaminergic interactions in various biological systems.

Etretinate-d3 is a deuterium-labeled derivative of Etretinate, a second-generation retinoid known for its therapeutic potential in severe psoriasis. This stable isotope can be utilized in metabolic studies and pharmacokinetic research to track Etretinate's behavior in biological systems. Its distinct isotopic signature supports precise analysis in various biochemical assays and advancements in dermatological research.

Sodium butyrate-d3 is a deuterium-labeled derivative of Sodium butyrate, functioning as an HDAC inhibitor. This compound exhibits anti-tumor activity and is useful in research involving epigenetic regulation and cancer biology. Sodium butyrate-d3 serves as a stable isotope for tracing studies and can be applied in investigations of metabolic pathways and cellular processes.

Adenosine-2′-13C is a stable isotope-labeled form of adenosine, which functions as a natural autacoid. It interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3, modulating a wide range of cellular physiological processes. This reagent is essential for studies involving metabolic pathways, receptor interaction assays, and biological labeling applications. Its use can enhance the understanding of adenosine's role in various biological contexts.

Deracoxib-d3 is a deuterated analog of Deracoxib, a selective COX-2 inhibitor. This compound primarily inhibits the COX-2 enzyme, effectively reducing prostaglandin production, and alleviates pain and inflammation, particularly following soft tissue surgeries in canine subjects. Additionally, Deracoxib has been shown to induce cell cycle arrest and apoptosis in tumor cells, demonstrating potential anti-tumor activity against conditions such as canine osteosarcoma, breast tumors, and bladder transitional cell carcinomas. As a stable isotope, Deracoxib-d3 is valuable in pharmacokinetic studies and biochemical research.

VR23-d8 is a deuterated analogue of VR23, designed as a stable isotope for research applications. This small molecule effectively inhibits trypsin-like proteasome activity with an IC50 of 1 nM, chymotrypsin-like proteasomes with an IC50 ranging from 50 to 100 nM, and exhibits an IC50 of 3 μM against caspase-like proteasomes. VR23-d8 is valuable for studies involving proteasomal function and regulation in various biological contexts.

5-Fluorouracil-13C4,15N2 is a stable isotope-labeled form of 5-Fluorouracil (5-FU), a uracil analog known for its potent antitumor properties. This compound primarily targets thymidylate synthetase, leading to the inhibition of pyrimidine synthesis and subsequent depletion of intracellular dTTP pools. As a result, 5-Fluorouracil-13C4,15N2 induces apoptosis in cancer cells and may serve as a chemical sensitizer in therapeutic applications. Additionally, it exhibits inhibitory effects against HIV, making it relevant for diverse biological research.

Rotenone-d3 is a deuterium-labeled derivative of Rotenone, a specific inhibitor of mitochondrial electron transport chain complex I. This compound is utilized in research to induce apoptosis by increasing the production of mitochondrial reactive oxygen species. Rotenone-d3 serves as a useful tool for studying mitochondrial function and the mechanisms of cell death in various biological systems.

Flurbiprofen-13C,d3 is a stable isotope-labeled form of Flurbiprofen, a nonsteroidal anti-inflammatory drug (NSAID) that exhibits potent antipyretic and analgesic properties. As a non-selective inhibitor of cyclooxygenase (COX), it plays a significant role in research related to inflammatory diseases such as osteoarthritis and rheumatoid arthritis, as well as studies concerning colorectal cancer. The incorporation of stable isotopes enables advanced analytical techniques in metabolic and pharmacokinetic investigations.

Rilmenidine-d4 is a deuterium-labeled derivative of Rilmenidine, a selective I1 imidazoline receptor agonist and antihypertensive agent. It exhibits key biological activities including the induction of autophagy and modulation of apoptosis through the pro-apoptotic protein Bax in human leukemic K562 cells. Rilmenidine also operates centrally to reduce sympathetic overactivity and affects renal function by inhibiting the Na+/H+ antiport. This stable isotope is valuable for pharmacokinetic studies and mechanistic investigations in cardiovascular and cancer research.

Triglycidyl Isocyanurate-d15 is a deuterated stable isotopomer of Triglycidyl Isocyanurate, a triazene triepoxide compound known for its antiangiogenic and antineoplastic properties. This reagent exhibits the ability to inhibit the proliferation of non-small-cell lung cancer cells through the activation of p53, leading to induced apoptosis. Triglycidyl Isocyanurate-d15 is an essential tool for cancer research, facilitating studies on molecular mechanisms and potential therapeutic applications in oncology.

Enterolactone-13C3 is a stable isotope-labeled form of Enterolactone, a bioactive phenolic metabolite derived from dietary lignans. This compound exhibits estrogenic properties and has demonstrated anti-breast cancer activity, serving as a radiosensitizer in human breast cancer cell lines. Its mechanism involves the inhibition of DNA repair and induction of apoptosis, making it a valuable tool for research on cancer biology and endocrine modulation.

L-Ascorbic acid-13C-1 is the stable isotope-labeled form of L-Ascorbic acid, primarily used as a biochemical tracer in metabolic studies. As an endogenous antioxidant, L-Ascorbic acid serves as an electron donor and has been shown to selectively inhibit Cav3.2 channels with an IC50 of 6.5 μM. Its ability to participate in collagen synthesis highlights its importance in research areas related to cellular metabolism, oxidative stress, and tissue repair.

Vandetanib-13C6 is a stable carbon isotope-labeled form of Vandetanib, which serves as a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity with an IC50 of 40 nM. In addition, it effectively inhibits the tyrosine kinase activity of VEGFR3/FLT4 (IC50 of 110 nM) and EGFR/HER1 (IC50 of 500 nM). This reagent is valuable for biological research applications involving cancer signaling pathways, pharmacokinetics, and biomarker studies.

Phenanthrene-13C2 is a stable isotope-labeled version of Phenanthrene, specifically incorporating two carbon-13 isotopes. As a polycyclic aromatic hydrocarbon (PAH), it is known to induce inflammation, oxidative stress, and apoptosis in biological systems. This compound is widely utilized in environmental research for the detection and assessment of PAH pollution, providing valuable insights into the impact of these contaminants on ecosystems and human health.

Tamoxifen-13C6 (ICI 47699-13C6) is a stable isotope-labeled variant of the selective estrogen receptor modulator (SERM), Tamoxifen (ICI 47699). This compound effectively blocks estrogen action in breast tissue while activating estrogenic pathways in other tissues such as bone, liver, and uterus. Additionally, it serves as a potent activator of the Hsp90 molecular chaperone, enhancing ATPase activity. Tamoxifen also demonstrates significant inhibitory effects against Ebola virus (EBOV Zaire) and Marburg virus (MARV) with IC50 values of 0.1 μM and 1.8 μM, respectively. Its biological activities include promoting autophagy, inducing apoptosis, and facilitating gene knockout in CreER transgenic mice, making it valuable for various research applications.

Paroxetine-d2 is a deuterium-labeled form of Paroxetine, a selective serotonin reuptake inhibitor (SSRI) that primarily targets serotonin transporters. This compound exhibits antidepressant, anti-anxiety, and analgesic properties, making it relevant for research on various psychological and chronic pain conditions. Additionally, Paroxetine has been shown to possess weak norepinephrine reuptake inhibition and potential anti-tumor activity through mechanisms such as inducing apoptosis in cancer cells. Its stable isotope nature allows for applications in pharmacokinetic studies and metabolic profiling.

Ramipril-d3 is the deuterated form of Ramipril, a potent angiotensin-converting enzyme (ACE) inhibitor with an IC50 value of 5 nM. This stable isotope-labeled compound is widely utilized in pharmacokinetic studies and biochemical research to trace metabolic pathways and assess the bioavailability of Ramipril. Its application in isotope labeling enhances the detection sensitivity in various analytical techniques, making it an essential tool for studying ACE inhibition and related therapeutic effects.

Dutasteride-13C6 is a stable isotope-labeled form of Dutasteride, a potent inhibitor of both isoforms of the enzyme 5α-reductase. By effectively blocking the conversion of testosterone to dihydrotestosterone (DHT), Dutasteride can play a significant role in the management of conditions such as benign prostatic hyperplasia and male pattern baldness. Additionally, due to its structural similarities to DHT, it may exhibit off-target effects on the androgen receptor, making it useful for a range of biological studies on androgen signaling pathways.

Saquinavir-d9 is a deuterium-labeled derivative of the HIV protease inhibitor Saquinavir. This stable isotope is utilized in research to study HIV-related mechanisms and therapeutic effects. In addition to its role in HIV protease inhibition, Saquinavir-d9 exhibits anti-inflammatory properties and can promote apoptosis in human red blood cells, making it a valuable tool for exploring various biological activities and applications within AIDS research.

Griseofulvin-13C,d3 is a stable isotope-labeled derivative of Griseofulvin, incorporating both carbon-13 and deuterium isotopes. This compound is widely utilized in metabolic studies and pharmacokinetic research to trace Griseofulvin's biological pathways and mechanisms of action. Its unique labeling allows for enhanced sensitivity and specificity in analytical techniques, making it a valuable tool in life science research.

5-Aminolevulinic acid-15N hydrochloride is a stable isotope-labeled derivative of 5-aminolevulinic acid, an essential intermediate in the heme biosynthesis pathway. As a universal precursor of tetrapyrroles, it plays a critical role in various biological processes. This reagent is useful for studies in metabolic pathways, tracing biosynthetic routes, and is commonly applied in research involving heme-related functions and disorders.

Vandetanib-d4 is a deuterium-labeled derivative of Vandetanib, a potent orally active inhibitor targeting VEGFR2/KDR tyrosine kinase with an IC50 of 40 nM. In addition to its primary action, Vandetanib exhibits inhibitory effects on VEGFR3/FLT4 and EGFR/HER1 with IC50 values of 110 nM and 500 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, drug metabolism research, and elucidating the pharmacological pathways of tyrosine kinase inhibitors.

2,4-Di-tert-butylphenol-d19 (2,4-DTBP-d19) is a deuterium-labeled variant of 2,4-Di-tert-butylphenol, a potent RXRα activator and human estrogen receptor ligand. This compound exhibits anti-inflammatory and antioxidant properties, with the ability to induce apoptosis in tumor cells. Additionally, it can activate RXRα in various receptor complexes and demonstrates antiviral and antifungal activities while showing promise in inhibiting Aβ-induced neurotoxicity. 2,4-DTBP-d19 serves as a valuable tool for research in cellular signaling, therapeutic development, and the synthesis of antioxidants and UV stabilizers.

Umbelliferone-13C6 (7-Hydroxycoumarin-13C6) is a stable isotope-labeled derivative of Umbelliferone, a naturally occurring coumarin compound. This reagent demonstrates significant biological activity, including inducing cell cycle arrest and apoptosis in HepG2 liver carcinoma cells. Research applications include investigations into its anticancer properties, neuroprotective effects, and potential as an anti-inflammatory and antioxidant agent. Additionally, Umbelliferone has shown to mitigate allergic airway inflammation and can effectively cross the blood-brain barrier, making it a valuable tool for various biochemical and pharmacological studies.