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      Suprofen (TN-762)
      Suprofen (TN-762)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1077
      CAS #: 40828-46-4Purity ≥98%

      Description: Suprofen (R25061; TN762;  R-25061; TN-762; Suprofen; Suprofenum; Profenal), a nonsteroid anti-inflammatory drug (NSAID), is a potent and nonselective dual inhibitor of COX-1/COX-2 enzymes with potential anti-inflammatory and antipyretic activity. It has been approved for use as a non-steroidal anti-inflammatory analgesic and antipyretic.  

      References: Drug Metab Dispos. 2003 Nov;31(11):1369-77; Am J Vet Res. 1996 Jun;57(6):875-8.

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      Molecular Weight (MW)260.31 
      FormulaC14H12O3S 
      CAS No.40828-46-4  
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 52 mg/mL (199.8 mM)
      Water: <1 mg/mL
      Ethanol: 52 mg/mL (199.8 mM)
      Solubility (In vivo)

      Chemical Name: 2-(4-(thiophene-2-carbonyl)phenyl)propanoic acid

      InChi Key: MDKGKXOCJGEUJW-UHFFFAOYSA-N

      InChi Code: InChI=1S/C14H12O3S/c1-9(14(16)17)10-4-6-11(7-5-10)13(15)12-3-2-8-18-12/h2-9H,1H3,(H,16,17)

      SMILES Code: CC(C1=CC=C(C(C2=CC=CS2)=O)C=C1)C(O)=O

      Synonyms

      R-25061;TN-762; R25061; TN 762;  R 25061; TN762; Suprofen; Suprofenum; Profenal


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      In Vitro

      In vitro activity: Suprofen inactivates the diclofenac-4-hydroxylase activity of baculovirus-expressed P450 2C9 in a time- and concentration-dependent manner, which is consistent with mechanism-based inactivation. Suprofen is a known generator of singlet oxygen whose participation in the reaction is supported by the effects of quenchers and scavengers. Suprofen photosensitizes the production of alkali-labile cleavage sites in DNA much more efficiently than direct strand breaks. Suprofen sensitizes photo-oxidation of cholesterol, producing 7 alpha- and 7 beta-hydroperoxides but not 5 alpha-hydroperoxide of cholesterol. Suprofen-sensitized photo-oxidation of membrane lipids of liposomes increases leakage of trapped glucose, suggesting photosensitized destabilization of the membrane structure. Suprofen incorporation in the phosphatidylcholine (PC) evaporation vesicles (REV) membrane leads to approximately 5% increase in the encapsulation efficiency (34%) in comparison to standard REV (29%).

      In VivoSuprofen combined with PGF2 alpha blocks induction of uterine contractions, suggesting the possibility that Suprofen also antagonizes PGF2 alpha receptor binding. Suprofen are effective at preventing BAB disruption after paracentesis in dogs, indicating their potential usefulness for treatment of prostaglandin-mediated ocular disease. Suprofen (3.7 mg/kg, i.v.) induces a marked decrease in the firing evoked in arthritic rats by ankle mobilization. 
      Animal modelRats
      Formulation & Dosage3.7 mg/kg, i.v.
      References

      Drug Metab Dispos. 2003 Nov;31(11):1369-77; Am J Vet Res. 1996 Jun;57(6):875-8. 

      These protocols are for reference only. InvivoChem does not independently validate these methods.

      Suprofen

      Time- and concentration-dependent loss of P450 2C9 diclofenac-4-hydroxylase activity after incubation with (±)-suprofen and NADPH. Drug Metab Dispos. 2003 Nov;31(11):1369-77.
      		 

      Suprofen

      Loss of P450 2C9 activity as a function of the ratio of (±)-suprofen to enzyme. Drug Metab Dispos. 2003 Nov;31(11):1369-77.
      		 

      Suprofen

      Substrate protection against P450 2C9 inactivation by (±)-suprofen. Drug Metab Dispos.2003 Nov;31(11):1369-77.

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