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Zaltoprofen COX inhibitor

Cat.No.S3008

Zaltoprofen(CN100,Soleton) is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
Zaltoprofen COX inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 298.36

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Quality Control

Batch: S300801 DMSO]60 mg/mL]false]Ethanol]31 mg/mL]false]Water]Insoluble]false Purity: 99.73%
99.73

Chemical Information, Storage & Stability

Molecular Weight 298.36 Formula

C17H14O3S

 Storage (From the date of receipt)
CAS No. 74711-43-6 Download SDF Storage of Stock Solutions

Synonyms CN100,Soleton Smiles CC(C1=CC2=C(C=C1)SC3=CC=CC=C3C(=O)C2)C(=O)O

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (201.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble

Molarity Calculator

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In vivo
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Mechanism of Action

Targets/IC50/Ki
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 this compound on bradykinin-induced responses of adult DRG neurons to investigate possible interaction sites. It most potently inhibits bradykinin-enhancement of capsaicin-induced Ca2+ uptake into DRG neurons. This chemical also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and the slow bradykinin-induced onset of substance P release from DRG neurons. [1] It produces an analgesic action on bradykinin-induced nociceptive responses by blocking the B(2) receptor-mediated pathway in the primary sensory neurons. This compound 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] It at 1nmol shows strong analgesic action on BK (i.pl.)-induced nociceptive flexor responses, whereas loxoprofen or its active metabolite loxoprofen-SRS does not. This chemical 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] It 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] This compound (10 mg/kg) administrated at 8 h after Con A treatment is found to inhibit the Con A-induced reduction in body weight. It (10 mg/kg) combined with Con A results in four times greater food intake than that in mice treated with only Con A. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11891529/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11494061/

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