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Tienilic AcidCayman Chemical Item Number 10008517 (CAS 40180-04-9) 
Tienilic Acid (CAS 40180-04-9)
Description
Cytochrome P450 enzymes function to metabolize both endogenous and exogenous compounds. Both the 3A and 2C isoforms are present in human liver of which CYP2C9 seems most highly expressed.1
Tienilic acid is a specific suicide substrate for CYP2C9 and CYP2C10 whereby its oxidation inactivates the enzyme.2,3 The time required to inactivate one half of the CYP2C10 enzyme at the maximal rate (t½max) is 3.4 minutes, with a dissociation constant (KI) value of 4.3 µM.3
1 Mancy, A., Broto, P., Dijols, S., et al. The substrate binding site of human liver cytochrome P450 2C9: An approach using designed tienilic acid derivatives and molecular modeling. Biochemistry 34 10365-10375 (1995).
2
Jean, P., Lopez-Garcia, P., Dansette, P.M., et al. Oxidation of tienilic acid by human yeast-
3
Lopez-Garcia, M.P., Dansette, P.M., and Mansuy, D. Thiophene derivatives as new mechanism-
Background ReadingJean, P., Lopez-Garcia, P., Dansette, P.M., et al. Oxidation of tienilic acid by human yeast- Mancy, A., Broto, P., Dijols, S., et al. The substrate binding site of human liver cytochrome P450 2C9: An approach using designed tienilic acid derivatives and molecular modeling. Biochemistry 34 10365-10375 (1995). Lopez-Garcia, M.P., Dansette, P.M., and Mansuy, D. Thiophene derivatives as new mechanism- Tienilic Acid is available in the following screening library: |
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Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins. |
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