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Carboxytolbutamide

Cat. No. M8841
Carboxytolbutamide Structure
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Quality Control & Documentation
Biological Activity

In vivo tolbutamide metabolite. Major urinary metabolite of tolbutamide.

Chemical Information
Molecular Weight 300.33
Formula C12H16N2O5S
CAS Number 2224-10-4
Solubility (25°C) methanol: soluble
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shotaro Uehara, et al. Methyl-hydroxylation and subsequent oxidation to produce carboxylic acid is the major metabolic pathway of tolbutamide in chimeric TK-NOG mice transplanted with human hepatocytes

[2] Shaoyu Zhang, et al. Liquid chromatography/tandem mass spectrometry method for simultaneous evaluation of activities of five cytochrome P450s using a five-drug cocktail and application to cytochrome P450 phenotyping studies in rats

[3] E NELSON, et al. Kinetics of carboxytolbutamide excretion following tolbutamide and carboxytolbutamide administration

[4] G Raghow, et al. High-performance liquid chromatographic assay of tolbutamide and carboxytolbutamide in human plasma

[5] D L Vesely. The comparative effects of tolbutamide and the non-hypoglycemic analog carboxytolbutamide on guanylate cyclase activity

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