Suicide substrate of CYP 2C9
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Tienilic Acid

Item No. 10008517

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-acetic acid
CAS Number
40180-04-9
Molecular Formula
C13H8Cl2O4S
Formula Weight
331.2
Purity
≥99%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/mlMethanol: 1 mg/ml
λmax
269, 295 nm
SMILES
O=C(C1=C(Cl)C(Cl)=C(OCC(O)=O)C=C1)C2=CC=CS2
InChi Code
InChI=1S/C13H8Cl2O4S/c14-11-7(13(18)9-2-1-5-20-9)3-4-8(12(11)15)19-6-10(16)17/h1-5H,6H2,(H,16,17)
InChi Key
AGHANLSBXUWXTB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $132

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    25 mg

    $351

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    50 mg

    $622

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    Product 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 (Kd) value of 4.3 µM.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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(33), 10365-10375 (1995).

    2. Jean, P., Lopez-Garcia, P., Dansette, P.M., et al. Oxidation of tienilic acid by human yeast-expressed cytochromes P450 2C8, 2C9, 2C18 and 2C19: Evidence that this drug is a mechanism-based inhibitor specific of cytochrome P450 2C9. Eur. J. Biochem. 241(3), 797-804 (1996).

    3. Lopez-Garcia, M.P., Dansette, P.M., and Mansuy, D. Thiophene derivatives as new mechanism-based inhibitors of cytochromes P450: Inactivation of yeast-expressed human liver P450 2C9 by tienilic acid. Biochemistry 33(1), 166-175 (1994).