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Cletoquine oxalate

Names

[ CAS No. ]:
14142-64-4

[ Name ]:
Cletoquine oxalate

[Synonym ]:
Cletoquine Oxalate

Biological Activity

[Description]:

Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine oxalate is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine oxalate is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine oxalate has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> Influenza Virus
Research Areas >> Infection
Research Areas >> Inflammation/Immunology

[Target]

Chikungunya virus (CHIKV)[2]


[In Vivo]

Hydroxychloroquine (5 mg/kg intravenously) is administered to BALB/c mice for blood and tissue to determine the content of Cletoquine (Desethylhydroxychloroquine). The tissue to blood concentration ratio (Kp) is ≥1, indicating accumulation of Cletoquine in tissues. The Cletoquine Kp ratio for the various tissues are observed in the descending order of liver (114.3)>kidney (24.4)>spleen (19.3)>lungs (16.5)>heart (5.5)[3].

[References]

[1]. Kumar M, et al. Molecular docking studies of chloroquine and its derivatives against P23pro-zbd domain of chikungunya virus: Implication in designing of novel therapeutic strategies. J Cell Biochem. 2019 Oct;120(10):18298-18308.

[2]. Charlier B, et al. Development of a novel ion-pairing HPLC-FL method for the separation and quantification of hydroxychloroquine and its metabolites in whole blood. Biomed Chromatogr. 2018 Aug;32(8):e4258.

[3]. Chhonker YS, et al. Simultaneous quantitation of hydroxychloroquine and its metabolites in mouse blood and tissues using LC-ESI-MS/MS: An application for pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Jan 1;1072:320-327.

Chemical & Physical Properties

[ Molecular Formula ]:
C18H24ClN3O5

[ Molecular Weight ]:
397.85300

[ Exact Mass ]:
397.14000

[ PSA ]:
131.78000

[ LogP ]:
2.67020

Related Compounds