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    Acemetacin (K-708; TVX 1322)
    Acemetacin (K-708; TVX 1322)

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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 #: V1057
    CAS #: 53164-05-9Purity ≥98%

    Description: Acemetacin (K708; Acemetacin; Rantudil; K-708; TVX 1322; TVX-1322) is a potent non-steroidal anti-inflammatory drug (NSAID) and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor with potential anti-inflammatory activity. Acemetacin is less potent than indomethacin in causing a concentration-related inhibition of PGE accumulation in gastric mucosal incubates. Acemetacin is also less potent than indomethacin in reducing gastric 6-keto-PGF1 alpha and TXB2.

    References: Int J Tissue React. 1993;15(2):49-53; Methods Find Exp Clin Pharmacol. 2010 Mar;32(2):101-5.

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    Molecular Weight (MW)415.82 
    FormulaC21H18ClNO6 
    CAS No.53164-05-9 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 83 mg/mL (199.6 mM) 
    Water: <1 mg/mL
    Ethanol: 58 mg/mL  (139.5 mM) 
    Other info

    Chemical Name: 1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, carboxymethyl ester

    InChi Key: FSQKKOOTNAMONP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C21H18ClNO6/c1-12-16(10-20(26)29-11-19(24)25)17-9-15(28-2)7-8-18(17)23(12)21(27)13-3-5-14(22)6-4-13/h3-9H,10-11H2,1-2H3,(H,24,25)

    SMILES Code: O=C(OCC(O)=O)CC1=C(C)N(C(C2=CC=C(Cl)C=C2)=O)C3=C1C=C(OC)C=C3

    SynonymsTVX1322; K-708; Acemetacin; Rantudil; K 708; TVX 1322; TVX-1322; K708


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    In Vitro

    In vitro activity: Acemetacin is less potent than indomethacin in causing a concentration-related inhibition of PGE accumulation in gastric mucosal incubates. Acemetacin is also less potent than indomethacin in reducing gastric 6-keto-PGF1 alpha and TXB2. Acemetacin probably exerts actions independent of conversion to Indomethacin, given the different effects of these two drugs on LTB(4) production. Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical trials. Acemetacin involves the sequential participation of nitric oxide (NO) or K+ channel pathways to confer its antinociceptive effect. Acemetacin exhibits the anti-inflammatory effect through PG synthesis inhibition. Acemetacin prevents the PGE2 release only at the high concentration of 10 μM in inflamed synovial tissue. Acemetacin exhibits less potent inhibitory effect on PGE2 release from the synovial membrane in the in vitro study.

    In VivoAcemetacin induces significantly less gastric and intestinal damage than indomethacin in rats pretreated with inhibitors of COX-2 and NOS, despite markedly suppressing COX activity. 
    Animal modelRats
    Formulation & DosageN/A
    References

    Int J Tissue React. 1993;15(2):49-53; Methods Find Exp Clin Pharmacol. 2010 Mar;32(2):101-5. 


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

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