Isotope-Labeled Compounds

Ketotifen-d3 fumarate is a deuterium-labeled derivative of Ketotifen fumarate, a second-generation noncompetitive H1-antihistamine and mast cell stabilizer. This compound is utilized primarily in research applications that require stable isotopes, enabling accurate studies in pharmacokinetics and metabolic pathways related to asthma and allergic reactions. Its stable isotope labeling enhances tracking and quantification in complex biological systems.

(Rac)-Levomepromazine-d3 hydrochloride is a labeled form of the racemic compound Methotrimeprazine, belonging to the phenothiazine class. This reagent exhibits antagonist activity at various neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin, and histamine receptors. It is primarily used as a stable isotope for research applications, enabling in-depth studies of pharmacological interactions and the metabolic pathways of related compounds.

Astemizole-d3 is a deuterium-labeled derivative of Astemizole, a second-generation antihistamine primarily functioning as a histamine H1-receptor antagonist, exhibiting an IC50 of 4 nM. This compound is not only effective in alleviating allergic symptoms but also possesses significant hERG K+ channel blocking activity, with an IC50 of 0.9 nM. Astemizole-d3 is valuable in pharmacokinetic studies and drug metabolism research, providing a stable isotope for tracing and quantitative analysis in biological systems.

Desloratadine-d5 is a deuterium-labeled analogue of Desloratadine, which is a selective H1-receptor antagonist. This compound is recognized for its efficacy in mitigating allergic responses and reducing inflammation. Desloratadine-d5 serves as a valuable tool in pharmacokinetic studies, isotopic labeling experiments, and the investigation of H1-antihistamine mechanisms in various biological systems.

Stavudine-d4 is a deuterium-labeled derivative of Stavudine, a potent nucleoside reverse transcriptase inhibitor (NRTI) targeting HIV-1 and HIV-2. This stable isotope is utilized in research applications to study metabolic processes and pharmacokinetics of Stavudine while minimizing background signal from natural isotopes. In addition, Stavudine is known to affect mitochondrial DNA replication, reduce NLRP3 inflammasome activation, modulate Amyloid-β autophagy, and induce apoptosis, making it a valuable tool for investigations into viral pathogenesis and cellular mechanisms.

Betamethasone-d5-1 is a deuterium-labeled derivative of Betamethasone, a synthetic glucocorticoid that exhibits potent anti-inflammatory and immunosuppressive properties. This compound is commonly utilized in research to study glucocorticoid signaling pathways, and its effects on gene regulation and apoptosis. Additionally, Betamethasone-d5-1 facilitates the investigation of fetal lung maturation and other developmental processes in biological systems.

Licofelone-d6 is a deuterium-labeled derivative of Licofelone, a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 0.21 µM and 0.18 µM, respectively. This compound demonstrates significant anti-inflammatory and anti-proliferative properties, making it relevant for research in osteoarthritis treatments. Licofelone-induced apoptosis and its ability to reduce the production of proinflammatory leukotrienes and prostaglandins further underscore its potential as a valuable tool in chemical biology.

Dapivirine-d4 is a deuterium-labeled analog of Dapivirine, a nonnucleoside reverse transcriptase inhibitor (NRTI) that targets HIV-1 reverse transcriptase. This compound serves as a stable isotope for various analytical applications, enhancing the study of Dapivirine metabolism and pharmacokinetics. Dapivirine demonstrates biological activities such as autophagy regulation and activation of signaling pathways, including Akt, Bad, and SAPK/JNK, making it relevant for research into HIV-1 treatment and cellular responses.

Imipramine-d3 hydrochloride is a deuterium-labeled analog of the tricyclic antidepressant imipramine, primarily classified as a stable isotope. This compound exhibits notable biological activity as a Fascin1 inhibitor with potential antitumor effects and acts as a serotonin transporter inhibitor with an IC50 value of 32 nM. Research applications include studies on autophagy induction in U-87MG glioma cells and apoptosis in HL-60 cells, as well as investigations into neuroprotective and immunomodulatory properties.

Uridine 5'-monophosphate-13C9,15N2 dilithium is a stable isotope-labeled form of uridine 5'-monophosphate, incorporating both 13C and 15N isotopes. This compound acts as an orally active mitochondrial ATP-dependent potassium channel activator, demonstrating cardioprotective effects. Additionally, uridine 5'-monophosphate promotes the synthesis of CDP-choline and induces apoptosis in intestinal epithelial cells, making it valuable for research in gut development and in studies related to gastrointestinal health.

Methyl 3,4-dihydroxybenzoate-d3-1 is a deuterium-labeled derivative of Methyl 3,4-dihydroxybenzoate, which serves as a stable isotope. This compound exhibits notable antioxidant and anti-inflammatory properties, making it significant in research related to the bioactivities of polyphenols. It is particularly useful in studies focused on metabolic pathways and the therapeutic potential of green tea-derived compounds.

Bendamustine-d8 is a deuterium-labeled derivative of Bendamustine, a purine analogue known for its powerful DNA cross-linking ability. This stable isotope facilitates the study of cancer research by enabling the tracking of Bendamustine's metabolism and efficacy in various biological systems. Bendamustine exhibits significant alkylating, anticancer, and antimetabolite properties, activating DNA-damage stress responses and apoptosis pathways, making it a valuable reagent for investigating cancer treatment modalities.

(±)-Enterodiol-d6 is a deuterium-labeled derivative of (±)-Enterodiol, a natural compound resulting from the microbial metabolism of lignans found in various dietary sources, including whole grains and vegetables. This stable isotope can be utilized in metabolic studies to trace the biodistribution and metabolic pathways of enterodiol in biological systems. In research, (±)-Enterodiol has been shown to induce apoptosis in colorectal cancer cells, highlighting its potential as an anticancer agent. Its applications extend to cancer research and the exploration of dietary impacts on human health.

Pomalidomide-d5 is a deuterium-labeled analog of Pomalidomide, a third-generation immunomodulatory agent. By acting as a molecular glue, Pomalidomide-d5 interacts with the E3 ligase cereblon, promoting the degradation of critical Ikaros transcription factors. This compound is valuable for studies in drug metabolism, pharmacokinetics, and mechanistic investigations related to multiple myeloma and other hematological malignancies.

Radotinib-d6 is a deuterium-labeled form of Radotinib, a selective inhibitor of the Bcr-Abl1 tyrosine kinase, recognized for its ability to penetrate the blood-brain barrier. With an IC50 of 34 nM, Radotinib exhibits significant anti-tumor activity, inhibiting cellular proliferation and inducing cell cycle arrest and apoptosis in tumor cells. This reagent is particularly valuable for research focused on chronic myeloid leukemia, multiple myeloma, and neurodegenerative conditions, including prion diseases.

Mitotane-d8 is a deuterated form of Mitotane, an antineoplastic agent predominantly used in the study of adrenocortical carcinoma. Mitotane exerts its adrenocorticolytic effects, in part, through inducing lipotoxicity via intracellular accumulation of free cholesterol. Additionally, it influences pituitary function by directly acting on corticotroph cells and activates CYP3A4 gene expression through the steroid and xenobiotic receptor (SXR). This stable isotope is valuable for pharmacokinetic studies and metabolic profiling in cancer research.

Rasagiline-13C3 mesylate is a stable isotope-labeled derivative of Rasagiline, which acts as a highly selective irreversible inhibitor of mitochondrial monoamine oxidase (MAO). It exhibits potent inhibition with IC50 values of 4.43 nM for rat brain MAO B and 412 nM for MAO A. This compound is primarily utilized in research related to neurodegenerative diseases and the study of MAO's role in neurotransmitter metabolism.

Perphenazine-d6 fumarate is a deuterated derivative of Perphenazine, primarily acting as a dopamine D2 and D3 receptor antagonist with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it demonstrates affinity for the 5-HT2A and Alpha-1A adrenergic receptors. This compound exhibits notable biological activities, including the inhibition of cancer cell proliferation and the induction of apoptosis. Perphenazine-d6 fumarate is useful in research addressing mental health disorders, cancer mechanisms, and inflammatory processes.

Griseofulvin-d3 is the deuterium-labeled form of Griseofulvin, a spirocyclic fungal metabolite known for its antifungal properties. It specifically targets fungal dermatophytes and is utilized in research related to antifungal efficacy and mechanisms of action. Griseofulvin-d3 serves as a valuable stable isotope for studies in pharmacokinetics and metabolic research involving antifungal agents.

Furazolidone-d4 is a deuterium-labeled derivative of the antibiotic furazolidone, primarily utilized as a stable isotope for biochemical research. This reagent allows for the accurate tracking and analysis of furazolidone metabolism and its interactions within biological systems. It serves as a valuable tool in pharmacokinetic studies and the investigation of antimicrobial mechanisms.

Galanthamine-O-methyl-d3 is a deuterium-labeled derivative of Galanthamine, a potent inhibitor of acetylcholinesterase (AChE) with an IC50 value of 500 nM. This stable isotope-labeled compound is primarily utilized in pharmacokinetic and metabolic studies. It serves as a valuable tool for investigating the pharmacological dynamics and biochemical pathways associated with cholinergic activity.

Noscapine-13C,d3 is a stable isotope-labeled form of noscapine, a phthalideisoquinoline alkaloid known for its potent antitussive properties. This compound primarily acts by engaging sigma opioid receptors and serves as a non-competitive inhibitor of bradykinin. In addition to its antitussive effects, noscapine disrupts microtubule dynamics, induces mitotic arrest, and promotes apoptosis, showcasing significant anticancer, neuroprotective, and anti-inflammatory activities. Its ability to cross the blood-brain barrier makes it suitable for a variety of biological research applications.

Demethoxycurcumin-d7 is a deuterium-labeled derivative of Demethoxycurcumin, a prominent active compound from turmeric. This reagent retains the anti-inflammatory properties characteristic of curcuminoids and demonstrates cytotoxic effects on human cancer cells through the induction of apoptosis. Demethoxycurcumin-d7 is valuable for research applications focused on cancer biology and the therapeutic potential of curcumin analogs.

Sulfaphenazole-d4 is a deuterium-labeled variant of Sulfaphenazole, which functions as a selective inhibitor of the cytochrome P450 2C9 enzyme. This compound exhibits cytoprotective properties by mitigating light-induced necrosis and apoptosis in photoreceptors, as well as providing bactericidal effects through the enhancement of M1 macrophage activity. Additionally, Sulfaphenazole has been shown to significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion, making it a valuable tool in cardiovascular and pharmacological research applications.

Carbaryl-d7 is a deuterium-labeled derivative of Carbaryl, which functions as an acetylcholinesterase inhibitor. By suppressing the breakdown of acetylcholine in the synaptic cleft, Carbaryl-d7 leads to an accumulation of acetylcholine, potentially resulting in neurotoxic effects. This stable isotope is primarily utilized in chemical research to study the enzymatic action and biological effects of Carbaryl and its derivatives.

Oleic Acid-13C-1 is a stable isotope-labeled form of oleic acid (9-cis-Octadecenoic acid) that serves as a versatile tracer in metabolic studies. This monounsaturated fatty acid is known to activate Na+/K+ ATPase, facilitating research into its role in cellular signaling and membrane potential regulation. Its application extends to studies in lipid metabolism, nutritional biochemistry, and other areas requiring precise tracking of fatty acid metabolism.

Mebendazole-d8 is a deuterium-labeled derivative of Mebendazole, which primarily targets helminths through its microtubule-disrupting mechanism. This stable isotope is utilized in research to study the pharmacokinetics and pharmacodynamics of Mebendazole and its interactions in biological systems. In addition, Mebendazole has been identified as a hedgehog signaling pathway inhibitor, making it valuable for studies in cancer research and developmental biology.

Chlorhexidine-d8 is a deuterium-labeled derivative of Chlorhexidine, a cationic antimicrobial agent known for its broad-spectrum activity against both Gram-positive and Gram-negative bacteria. Its primary mechanism involves binding to microbial cell membrane phospholipids, leading to structural disruption and leakage of cellular contents. This compound is utilized in a variety of research applications, including studies on antimicrobial resistance, cell membrane integrity, and the metabolic pathways of bacteria. Chlorhexidine-d8 serves as a valuable stable isotope for advanced analytical techniques in chemical research.

L-Asparagine-1,2,3,4-13C4 monohydrate is a stable isotope-labeled form of the amino acid L-asparagine. This compound serves as a substrate for L-asparaginase, an enzyme critical in the treatment of leukemia, which depletes asparagine and glutamine levels to inhibit protein biosynthesis and promote apoptosis in lymphoblasts. L-Asparagine-1,2,3,4-13C4 monohydrate has applications in research involving acute lymphoblastic leukemia, functioning as a biomarker and enabling detailed studies of metabolic pathways related to cancer cell growth and survival.

Ketoprofen-13C,d3 is a stable isotope-labeled form of Ketoprofen, a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits cyclooxygenase (COX) enzymes. It exhibits potent inhibition, with IC50 values of 2 nM for COX-1 and 26 nM for COX-2 in human blood monocytes. This labeled compound is valuable for metabolic studies, pharmacokinetic research, and tracing biological pathways involving Ketoprofen.

Adenosine-3′-13C is a stable isotope-labeled form of adenosine, an important endogenous autacoid that interacts with four G protein-coupled receptors: A1, A2A, A2B, and A3. This compound plays a crucial role in various physiological processes, including modulation of neurotransmission, vascular regulation, and immune response. Adenosine-3′-13C is valuable for metabolic studies and tracer experiments, allowing researchers to track adenosine's role in cellular signaling and energy metabolism in various biological systems.

(R)-(+)-Verapamil-d6 hydrochloride is a deuterium-labeled derivative of (R)-Verapamil hydrochloride, serving as a stable isotope. This compound primarily functions as a P-glycoprotein inhibitor and effectively blocks MRP1-mediated transport. Its biological activity makes it a valuable tool for research in chemosensitization of MRP1-overexpressing cells to various anticancer agents, enhancing the understanding of drug resistance mechanisms in cancer therapy.

2-Methoxyestradiol-13C,d3 is a stable isotope-labeled version of 2-Methoxyestradiol, an endogenous metabolite of 17β-estradiol. It functions primarily as an apoptosis inducer and angiogenesis inhibitor, demonstrating significant antineoplastic properties. Additionally, 2-Methoxyestradiol destabilizes microtubules and acts as a potent inhibitor of superoxide dismutase (SOD), generating reactive oxygen species (ROS) that can induce autophagy in various cancer cell lines such as HEK293, U87, and HeLa. This reagent is valuable for research in cancer biology and the mechanisms of estrogen metabolism.

Minocycline-d6 is a deuterium-labeled form of Minocycline, a semi-synthetic tetracycline antibiotic known for its ability to penetrate the blood-brain barrier. It acts primarily as a hypoxia-inducible factor (HIF)-1α inhibitor and exhibits anti-cancer, anti-inflammatory, and glutamate antagonistic properties. The compound effectively reduces glutamate neurotransmission, offering neuroprotective and antidepressant effects. Additionally, Minocycline inhibits bacterial protein synthesis by binding to the 30S subunit of the bacterial ribosome, producing a bacteriostatic effect. This reagent is suitable for research in pharmacology, neuroscience, and cancer biology.

Diatrizoic acid-d6 is a deuterium-labeled version of the iodinated radiocontrast agent, Diatrizoic acid. This stable isotope is primarily used in radiographic imaging applications, particularly for visualizing the airways. Diatrizoic acid is known to induce mitochondrial turnover and oxidative stress, leading to apoptosis through calcium dysregulation. Its isotopic labeling facilitates enhanced tracking and analysis in various biochemical studies.

Mebendazole-d3 is a deuterium-labeled form of Mebendazole, designed as a stable isotope for research applications. It primarily targets the tubulin protein, disrupting microtubule polymerization, which is crucial for many cellular processes. This compound is utilized in pharmacokinetic studies and metabolic research to trace the pharmacodynamics and distribution of Mebendazole in biological systems.

Formamide-d3 is the deuterated form of formamide, recognized for its role as a stable isotope. It primarily serves as a potent DNA denaturant, effectively destabilizing DNA structures in various buffer solutions. Furthermore, formamide-d3 has applications in decalcifying rat cardiac cells and is utilized as a solvent and chemical precursor in the synthesis of ion compounds, resins, and plasticizers, making it valuable for diverse biological and chemical research applications.

Trametinib-13C,d3 is a stable isotope-labeled analog of Trametinib, a potent MEK1 and MEK2 inhibitor. With an IC50 of approximately 2 nM, Trametinib is known to activate autophagy and induce apoptosis in various cellular models. This labeled compound is ideal for use in metabolic studies, pharmacokinetic research, and tracer studies involving MEK signaling pathways.

Dapivirine-d11 is a deuterium-labeled derivative of Dapivirine, a nonnucleoside reverse transcriptase inhibitor (NRTI) that specifically targets HIV-1 reverse transcriptase. This stable isotope-labeled compound is utilized in research to investigate the metabolic pathways and pharmacokinetics of Dapivirine. Additionally, Dapivirine has been shown to modulate autophagy and activate key signaling molecules such as Akt, Bad, and SAPK/JNK, making it relevant for studies in HIV therapy and cellular response mechanisms.

D-Mannitol-d is a deuterium-labeled form of D-Mannitol, a polyol with significant applications in both food and pharmaceutical research. It functions primarily as an osmotic diuretic, utilized to alleviate tissue edema, while also promoting the absorption of calcium and magnesium through cecal fermentation. Additionally, D-Mannitol-d is instrumental in studies related to metabolic processes, including the induction of brown fat formation via β3-adrenergic receptor activation, potentially contributing to improved insulin sensitivity and reduced blood glucose levels. Its unique properties make it valuable for maintaining osmotic pressure in plant cell cultures, particularly when cellular integrity is compromised.

Tebufenozide-d9 is a deuterium-labeled analog of Tebufenozide, which acts as a nonsteroidal ecdysone agonist. This compound is primarily utilized in pest control and exhibits significant cytotoxic effects, inducing apoptosis in HeLa and insect Tn5B1-4 cell lines. Its stable isotope labeling enables advanced studies in metabolic tracking and pesticide biology.

Propylparaben-d7 is a deuterium-labeled derivative of Propylparaben (Propyl parahydroxybenzoate), functioning as a stable isotope for analytical studies. This compound acts as an antimicrobial preservative, commonly utilized in cosmetics, pharmaceuticals, and food products. Research has demonstrated that Propylparaben interferes with antral follicle growth and alters steroidogenic function by impacting cell-cycle, apoptosis, and steroidogenesis pathways. Additionally, studies in rodent models indicate that Propylparaben may reduce sperm count and motility, making it pertinent for investigations into reproductive health effects.

Dacarbazine-d6 is a deuterated form of Dacarbazine, an antineoplastic agent primarily targeting DNA synthesis. It exhibits significant cytotoxic activity against melanoma cells, making it valuable for cancer research and therapeutic studies. The stable isotope labeling allows for improved tracking and analysis in pharmacokinetic studies and metabolic research.

Mitotane-13C12 (2,4′-DDD-13C12) is a stable isotope-labeled form of Mitotane, an antineoplastic agent primarily utilized in the study of adrenocortical carcinoma. This compound exerts its adrenocorticolytic effects through mechanisms involving lipotoxicity and the accumulation of intracellular free cholesterol. Additionally, Mitotane influences endocrine functions by affecting corticotroph cells in the pituitary and induces CYP3A4 gene expression via activation of the steroid and xenobiotic receptor (SXR). This reagent is valuable for metabolic and pharmacokinetic studies in cancer research.

Rabeprazole-d3 sodium is a deuterium-labeled form of the second-generation proton pump inhibitor, Rabeprazole sodium, which irreversibly inhibits the gastric H+/K+-ATPase. This compound has been shown to induce apoptosis and acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 value of 0.3 μM. Rabeprazole-d3 sodium is utilized in research involving gastric ulcerations and gastroesophageal reflux disorders.

Metformin-d6 (1,1-Dimethylbiguanide-d6) serves as a stable isotope-labeled version of Metformin, which primarily targets the mitochondrial respiratory chain in the liver. This compound is critical for studies on type 2 diabetes management due to its role in activating AMPK, thus enhancing insulin sensitivity. Additionally, Metformin-d6 contributes to understanding glucose regulation through the inhibition of Rap1 in SF1 hypothalamic neurons. Its utility extends to investigating liver oxidative stress and the modulation of autophagy-related proteins via AMPK activation and mTOR inhibition, making it relevant for evaluating renal cell carcinoma growth in both in vitro and in vivo settings.

Oxcarbazepine-d10 is a deuterated form of Oxcarbazepine, primarily known for its role as a sodium channel blocker. This compound exhibits significant anti-cancer properties, effectively inhibiting glioblastoma cell proliferation while promoting apoptosis or G2/M phase arrest in glioblastoma cell lines. Oxcarbazepine-d10 is utilized in research to study the mechanisms of action and therapeutic applications in cancer and epilepsy.

Ligustrazine-d12 is a deuterium-labeled derivative of Ligustrazine, an alkylpyrazine compound derived from Ligusticum chuanxiong Hort. This stable isotope serves as a valuable tool in metabolic studies and isotope tracing applications. Ligustrazine is known for its potential nootropic and anti-inflammatory properties in preclinical models, making Ligustrazine-d12 relevant for research in neuropharmacology and inflammation pathways.

Thioridazine 2-Sulfone-d3 is a stable isotope-labeled analog of Thioridazine hydrochloride, an antagonist of the dopamine D2 receptor family. This compound demonstrates significant anti-psychotic and anti-anxiety properties and exerts potent inhibition of the PI3K-Akt-mTOR signaling pathway, contributing to its anti-angiogenic effects. Additionally, Thioridazine hydrochloride has been shown to induce antiproliferative effects and promote apoptosis in various cancer cell types, particularly targeting cancer stem cells (CSCs), making it a valuable tool for cancer research and neurological studies.

Oxcarbazepine-d4 is a deuterium-labeled analog of Oxcarbazepine, a sodium channel blocker. This compound exhibits significant anti-cancer properties by inhibiting glioblastoma cell growth and inducing apoptosis or G2/M cell cycle arrest in glioblastoma cell lines. Oxcarbazepine-d4 is valuable for research in cancer therapeutics and anticonvulsant studies.