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Tienilic Acid

Cayman Chemical Item Number 10008517

(CAS 40180-04-9)

Tienilic Acid (CAS 40180-04-9)

See more	Cytochrome P450 (88) Metabolism (139)

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 (t_½max) 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-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 241 797-804 (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 33 166-175 (1994).

Formal Name	[2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-acetic acid
CAS Number	40180-04-9
Molecular Formula	C₁₃H₈Cl₂O₄S
Formula Weight	331.2
Formulation	A crystalline solid
Purity	>99%
λ_max	295 nm
Stability	1 year
Storage	4°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard O=C(C1=C(Cl)C(Cl)=C(OCC(O)=O)C=C1)C2=CC=CS2

Background Reading

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 241 797-804 (1996).

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-based inhibitors of cytochromes P450: Inactivation of yeast-expressed human liver P450 2C9 by tienilic acid. Biochemistry 33 166-175 (1994).

Tienilic Acid is available in the following screening library:

Bio-active Lipid I Screening Library (96-Well)

Size	Price	Quantity	Subtotal
5 mg	$58.00		$0.00
10 mg	$110.00		$0.00
25 mg	$261.00		$0.00
50 mg	$464.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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