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Carbazeran citrate

Names

[ CAS No. ]:
153473-94-0

[ Name ]:
Carbazeran citrate

[Synonym ]:
1-(6,7-Dimethoxy-1-phthalazinyl)-4-piperidinyl ethylcarbamate 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Carbamic acid, N-ethyl-, 1-(6,7-dimethoxy-1-phthalazinyl)-4-piperidinyl ester, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) (salt)

Biological Activity

[Description]:

Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Metabolic Disease

[Target]

phosphodiesterase[1]


[In Vivo]

Carbazeran (10 mg/kg; p.o.) (citrate) of the unmetabolized in samples from humanized-liver mice, the mean plasma concentrations are lower than in those from control mice for 0.5~4 hours after oral administration[1]. Oral administration of carbazeran (citrate) to guinea pigs has reportedly resulted in large kinetic deuterium isotope effects on the AUC and Cmax, without a change of systemic half-life[1]. Animal Model: Mice[1] Dosage: 10 mg/kg Administration: P.o. Result: The mean plasma concentrations were lower than in those from control mice for 0.5~4 hours after oral administration.

[References]

[1]. Uehara S, et al. Human Aldehyde Oxidase 1-Mediated Carbazeran Oxidation in Chimeric TK-NOG Mice Transplanted with Human Hepatocytes. Drug Metab Dispos. 2020;48(7):580-586.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H32N4O11

[ Molecular Weight ]:
552.531

[ Exact Mass ]:
552.206787


Related Compounds

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