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    Zaltoprofen (CN100)
    Zaltoprofen (CN100)

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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 #: V1069
    CAS #: 74711-43-6Purity ≥98%

    Description: Zaltoprofen (CN 100; CN-100; CN100), a nonsteroidal anti-inflammatory drug (NSAID), is a potent inhibitor of COX-1 and COX-2 enzymes with potential anti-inflammatory activity. It has been approved for treatment of arthritis. It acts by binding to specific sites on the bradykinin B2 receptor. Zaltoprofen most potently inhibits bradykinin-enhancement of capsaicin-induced Ca2+ uptake into DRG neurons. Zaltoprofen also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and the slow bradykinin-induced onset of substance P release from DRG neurons.

    References: Neuropharmacology. 2005 Jun;48(7):1035-42; Int J Mol Med. 2002 Apr;9(4):369-72.

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    Molecular Weight (MW)298.36 
    FormulaC17H14O3S 
    CAS No.74711-43-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 60 mg/mL (201.1 mM) 
    Water: <1 mg/mL
    Ethanol: 31 mg/mL (103.9 mM)
    Other info

    Chemical Name: 10,11-Dihydro-alpha-methyl-10-oxodibenzo(b,f)thiepin-2-acetic acid

    InChi Key: MUXFZBHBYYYLTH-UHFFFAOYSA-N

    InChi Code: InChI=1S/C17H14O3S/c1-10(17(19)20)11-6-7-15-12(8-11)9-14(18)13-4-2-3-5-16(13)21-15/h2-8,10H,9H2,1H3,(H,19,20)

    SMILES: O=C(O)C(C)C1=CC=C(C(C2)=C1)SC3=CC=CC=C3C2=O

    SynonymsCN 100; CN-100; CN100


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    In Vitro

    In vitro activity: Zaltoprofen binds to specific sites on the protein of the bradykinin B2 receptor, hence we have examined the effect of zaltoprofen on bradykinin-induced responses of adult DRG neurons to investigate possible interaction sites. Zaltoprofen most potently inhibits bradykinin-enhancement of capsaicin-induced Ca2+ uptake into DRG neurons. Zaltoprofen also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and the slow bradykinin-induced onset of substance P release from DRG neurons. Zaltoprofen produces an analgesic action on bradykinin-induced nociceptive responses by blocking the B(2) receptor-mediated pathway in the primary sensory neurons. Zaltoprofen completely inhibits the bradykinin-induced increase of [Ca(2+)](i), which is inhibited by B(2) antagonist D-Arg-[Hyp(3), Thi(5,8), D-Phe(7)]-bradykinin, but not by B(1) antagonist. Zaltoprofen at 1nmol shows strong analgesic action on BK (i.pl.)-induced nociceptive flexor responses, whereas loxoprofen or its active metabolite loxoprofen-SRS does not. Zaltoprofen also inhibits the nociception induced by [Tyr8]-BK, a specific agonist of B2-type BK receptor, but does not affect the nociception by [Lys-des-Arg9]-BK, a specific agonist of B1-type BK receptor. Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) causes potent inhibition of cyclooxygenase-2 with fewer side effects on the gastrointestinal tract.

    In VivoZaltoprofen improves the loss in body weight in both Con A-treated mice and carbon tetrachloride-treated rats. Zaltoprofen (10 mg/kg) administrated at 8 h after Con A treatment is found to inhibit the Con A-induced reduction in body weight. Zaltoprofen (10 mg/kg) combined with Con A results in four times greater food intake than that in mice treated with only Con A. 
    Animal modelMice and rats
    Formulation & Dosage10 mg/kg
    References

    Neuropharmacology. 2005 Jun;48(7):1035-42; Int J Mol Med. 2002 Apr;9(4):369-72. 


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

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