Zaltoprofen

SKU: orb1300513

Description

Zaltoprofen

Research Area

Immunology & Inflammation, Neuroscience

Key Properties

• CAS Number: 74711-43-6
• MW: 298.36
• Purity: 99.72%
• Formula: C₁₇H₁₄O₃S
• SMILES: CC(C(O)=O)C1=CC2=C(SC3=CC=CC=C3C(=O)C2)C=C1
• Target: COX
• Solubility: DMSO:75 mg/mL (251.37 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:29 mg/mL (97.2 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.7 mM)

Bioactivity

• Target IC50:
  COX-2:0.34 μM (IC50)|COX-1:1.3 μM (IC50)
• In Vivo:
  After 8 hours of ConA treatment, mice were administrated of Zaltoprofen(10 mg/kg) resulting in inhibition of ConA-induced body weight loss. The combination of 10 mg/kg Zaltoprofen and ConA resulted in a 4-fold increase in food intake in mice compared to ConA only. Therefore, Zaltoprofen increased weight loss in ConA-treated mice.
• In Vitro:
  Zaltoprofe is a non-steroidal anti-inflammatory drug (NSAID) that effectively inhibits cyclooxygenase-2 with minimal side effects on the gastrointestinal tract. Zaltoprofe binds to a specific site of the bradykinin B2 receptor protein, therefore, the effect of Zaltoprofen on the bradykinin-evoked response of adult DRG neurons can be investigated to investigate possible interaction sites. Zaltoprofen is the most effective inhibitor of bradykinin enhancing capsaicin-induced Ca2+ uptake into DRG neurons. Zaltoprofen also significantly inhibits bradykinin-induced 12-lipoxygenase (12-LOX) activity and slow bradykinin-induced release of the substance P from DRG neurons. Zaltoprofe showed a potent analgesic effect on BK (i.pl.)-induced hyperalgesia at 1 nmol, whereas loxoprofen or its active metabolite loxoprofen-SRS did not. Zaltoprofe also inhibits [Tyr8]-BK-induced nociception in that it is a type B2 receptor specific agonist; but does not affect the nociception induced by [lysine-DES-Arg9]-BK, which is type B1 BK receptor specific agonist. In primary sensory neurons, Zaltoprofe produces an analgesic effect of a bradykinin-induced nociceptive response by blocking the B(2) receptor-mediated pathway. Zaltoprofe completely inhibits Ca2+ increase induced by bradykinin, which is inhibited by the B(2) antagonist D-Arg-[Hyp(3), Thi(5,8), D-Phe(7)]-bradykinin, but not B(1) Antagonist.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

anti-inflammatory, analgesic, Cyclooxygenase, COX-2, COX-1, COX, CN 100, CN100, CN-100, Inhibitor, inhibit, non-steroidal, NSAID, Soleton, Zaltoprofen

Compound Identifiers

PubChem CID

5720