Zaltoprofen

Catalog No.S3008

Zaltoprofen Chemical Structure

Molecular Weight(MW): 298.36

Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 770 In stock
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Biological Activity

Description Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
Targets
COX-1 [1] COX-2 [1]
In vitro

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. [1] 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. [2] 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. [3] Zaltoprofen is a non-steroidal anti-inflammatory drug (NSAID) causes potent inhibition of cyclooxygenase-2 with fewer side effects on the gastrointestinal tract.[4]

In vivo Zaltoprofen improves the loss in body weight in both Con A-treated mice and carbon tetrachloride-treated rats. [4] 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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 60 mg/mL (201.09 mM)
Ethanol 31 mg/mL (103.9 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 298.36
Formula

C17H14O3S

CAS No. 74711-43-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01369238 Unknown status Whiplash Injuries Korean Pharmacoacupuncture Institute June 2011 --

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COX Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID