NS-398

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NS-398  纯度: 98.70%

NS-398 是一种非甾体类抗炎剂,具有解热作用,可用于缓解疼痛的研究。NS-398 能够选择性地抑制 COX-2 的活性,IC50 值为 3.8 μM,在 100 μM 的浓度下,对 COX-1 的活性没有作用。

NS-398

NS-398 Chemical Structure

CAS No. : 123653-11-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥700 In-stock
50 mg ¥2260 In-stock
100 mg ¥3500 In-stock
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生物活性

NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.

IC50 & Target

COX-2

3.8 μM (IC50)

体外研究
(In Vitro)

NS-398 is a non-steroidal an-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM[1]. NS-398 weakly inhibits PG endoperoxide synthase activity from sheep seminal vesicle microsomes (IC50, 11 μM)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NS-398 (0.5-10 mg/kg, p.o.) dose-dependently inhibits paw edema in rats, with an ED30 of 1.14 mg/kg, shows therapeutic effects on adjuvant arthritis (ED30, 4.69 mg/kg), exhibits dose-dependent analgesic activity (ED50, 1.65 mg/kg), and has antipyretic effect (ED50, 1.84 mg/kg) in rats. In mice, NS-398 suppresses writhing reactions induced by acetic acid with an ED50 of 8.2 mg/kg[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

314.36

Formula

C13H18N2O5S

CAS 号

123653-11-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 9 mg/mL (28.63 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1811 mL 15.9053 mL 31.8107 mL
5 mM 0.6362 mL 3.1811 mL 6.3621 mL
10 mM 0.3181 mL 1.5905 mL 3.1811 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.95 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.95 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Futaki N, et al. NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins. 1994 Jan;47(1):55-9.

    [2]. Futaki N, et al. NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesions. Gen Pharmacol. 1993 Jan;24(1):105-10.

Animal Administration
[2]

Mice[2]
Briefly, male ddy mice weighing about 30 g are used. The writhing syndrome is induced by injecting 0.75% of acetic acid, intraperitoneally. Ten minutes later, the number of writhings are counted for the next 10 min. NS-398 is administered orally 30 min prior to the injection. The analgesic effect is expressed as % of inhibition, compared with the vehicle-treated control[2].
Rats[2]
Briefly, male Lewis rats weighing about 160 g are used. Arthritis is induced by injecting 0.1 mL of 0.7% Mycobacterium tubercu-losis-liquid paraffin into the left hind paw. On day 15, the rats are grouped according to the degree of secondary lesions in the right hind paw. NS-398 is administered orally once daily from days 15 to 18. Foot volume is measured on day 19. Relative edema volume (REV) is calculated for each animal[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Futaki N, et al. NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins. 1994 Jan;47(1):55-9.

    [2]. Futaki N, et al. NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesions. Gen Pharmacol. 1993 Jan;24(1):105-10.

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