您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Zaltoprofen
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Zaltoprofen
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Zaltoprofen图片
CAS NO:74711-43-6
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Soleton
扎托布洛芬
CN100
产品介绍
Zaltoprofen 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。

产品描述

Zaltoprofen is a Cox-1 and Cox-2 inhibitor, which is used for the treatment of arthritis.

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.

Cas No.

74711-43-6

分子式

C17H14O3S

分子量

298.36

别名

Soleton;扎托布洛芬;CN100

储存和溶解度

H2O:<1 mgml
Ethanol:29 mg/mL (97.2 mM)
DMSO:56 mg/mL (187.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years