21840-08-4
Chemical Structure
Melarsen oxide
- CAS No.: 21840-08-4
- Formula:C9H9AsN6O
- Molecular Weight:292.13
IUPAC Name: N2-(4-(oxoarsanyl)phenyl)-1,3,5-triazine-2,4,6-triamine
InChIKey: YDKGKLBKFOIXPU-UHFFFAOYSA-N
SMILES: O=[As]C1=CC=C(NC2=NC(N)=NC(N)=N2)C=C1
Biological Activity: Melarsen oxide is a blood-brain barrier-permeable, competitive antimalarial agent and Glutathione reductase inhibitor with a Ki of 23.7 μM. Melarsen oxide induces rapid lysis of bloodstream-form Trypanosoma brucei cells by disrupting the plasma membrane. Melarsen oxide exhibits trypanocidal activity against Trypanosoma brucei rhodesiense. Melarsen oxide is applicable to research related to filariasis and African trypanosomiasis[1][2][3].
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Melarsen oxide | Melarsen oxide is a blood-brain barrier-permeable, competitive antimalarial agent and Glutathione reductase inhibitor with a Ki of 23.7 μM. Melarsen oxide induces rapid lysis of bloodstream-form Trypanosoma brucei cells by disrupting the plasma membrane. Melarsen oxide exhibits trypanocidal activity against Trypanosoma brucei rhodesiense. Melarsen oxide is applicable to research related to filariasis and African trypanosomiasis. | |||||||||||||||||||||
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References
- [1]. Müller S, et al. Differential susceptibility of filarial and human erythrocyte glutathione reductase to inhibition by the trivalent organic arsenical melarsen oxide. Molecular and biochemical parasitology. 1995 May;71(2):211-9.
- [2]. Gould MK, et al. Propidium iodide-based methods for monitoring drug action in the kinetoplastidae: comparison with the Alamar Blue assay. Analytical biochemistry. 2008 Nov 15;382(2):87-93.
- [3]. Keiser J, et al. Investigations of the metabolites of the trypanocidal drug melarsoprol. Clinical pharmacology and therapeutics. 2000 May;67(5):478-88.
