Cycloguanil-d6 nitrate
Based on 1 publication(s) in Google Scholar
Cycloguanil-d6 (Chlorguanide triazine-d6) nitrate is the deuterium labeled Cycloguanil nitrate. Cycloguanil nitrate is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil nitrate blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil nitrate inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil nitrate also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.
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- CAS No.: 2070015-19-7
- Formule: C11H9D6ClN6O3
- Masse moléculaire:320.77
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cycloguanil-d6 nitrate
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Activité biologique
Description
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Application
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2070015-19-7
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Unlabeled CAS 516-21-2
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Appearance Solid
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Masse moléculaire 320.77
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Formule C11H9D6ClN6O3
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Color White to off-white
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SMILES
[N+](O)(=O)[O-].C1(Cl)C=CC(N2C(C([2H])([2H])[2H])(C([2H])([2H])[2H])N=C(N)N=C2N)=CC=1
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Synonyms
Chlorguanide triazine-d6 nitrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Drug Metab Pharmacokinet
Physiologically based pharmacokinetic model analysis of the inhibitory effect of vonoprazan on the metabolic activation of proguanil. [Abstract]2024 Feb:54:100537. PMID: 38086197
Pureté et documentation
Références
[1]. Matthaei J, et al. OCT1 Deficiency Affects Hepatocellular Concentrations and Pharmacokinetics of Cycloguanil, the Active Metabolite of the Antimalarial Drug Proguanil. Clin Pharmacol Ther. 2019;105(1):190-200. [Content Brief]
[2]. Brown JI, et al. Cycloguanil and Analogues Potently Target DHFR in Cancer Cells to Elicit Anti-Cancer Activity. Metabolites. 2023;13(2):151. Published 2023 Jan 19. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cycloguanil-d6 nitrate Related Classifications
HY-12784S1 Related Classifications
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