扎托布洛芬 T6737

Product Introduction
Bioactivity


英文名: Zaltoprofen

描述: Zaltoprofen (Soleton) 是一种非甾体类抗炎剂，具有强大的抗炎作用和对炎性疼痛的止痛作用。它是可口服的COX-2抑制剂，对COX-1和COX-2的IC50值分别为 1.3 和 0.34 μM。

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 29 mg/mL (97.2 mM)
DMSO : 56 mg/mL (187.7 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: anti-inflammatory | CN-100 | COX-2 | inhibit | non-steroidal | Inhibitor | COX | NSAID | COX-1 | Cyclooxygenase | Zaltoprofen | analgesic | CN 100

相关产品: (-)-Pinoresinol | Ginsenoside Rg5 | Revaprazan hydrochloride | Pemedolac | Gaultherin | Benoxaprofen | syringaldehyde | Minoxidil | Meclofenamic acid sodium | Murrangatin

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Pyroptosis Compound Library | Angiogenesis related Compound Library | Mitochondria-Targeted Compound Library | Anti-Cancer Drug Library | Neuronal Signaling Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Nonsteroidal Anti-Inflammatory Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途