NS 398
(Synonyms: 抑制剂) 目录号 : GC12241
A selective COX2 inhibitor
Cas No.:123653-11-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Animal experiment: |
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]. |
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References: [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. |
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NS 398 is a selective inhibitor of cyclooxygenase-2 with IC50 value of 3.8 μM [1].
Cyclooxygenase (COX) is an enzyme that is responsible for the formation of prostaglandins, prostacyclin and thromboxane. COX-2 converts arachidonic acid (AA) to prostaglandin endoperoxide H2.
NS 398 is a selective COX-2 inhibitor and a novel anti-inflammatory agent. NS 398 inhibited COX-2 with IC50 value of 3.8 μM in a concentration-dependent way [1]. In RG/C2, AA/C1 and RR/C1 pre-malignant human colorectal adenoma cell lines, NS-398 (20 ~ 100 μM) inhibited cell proliferation and induced apoptosis. In HT29 colorectal carcinoma cell lines, NS-398 induced apoptosis. Also, NS-398 increased COX-2 protein expression. In HT29 cultures, NS-398 inhibited prostaglandin E2 secretion and COX-2 activity [2].
In rats with trauma, NS-398 (0.3-5 mg/kg) exhibited anti-inflammatory and analgesic effects [1]. In Balb/C mice, NS-398 (10 mg/kg) reduced prostaglandin E2 (PGE2) production and also significantly decreased the production of NO, IL-6 and TNF-α. Also, NS-398 decreased the mRNA levels of COX-2 and inhibited NF-κB activation. These results suggested that NS-398 regulated the inflammatory response after trauma and improved survival [3].
References:
[1]. Futaki N, Takahashi S, Yokoyama M, et al. NS-398, a new anti-inflammatory agent, selectively inhibits prostaglandin G/H synthase/cyclooxygenase (COX-2) activity in vitro. Prostaglandins, 1994, 47(1): 55-59.
[2]. Elder DJ, Halton DE, Crew TE, et al. Apoptosis induction and cyclooxygenase-2 regulation in human colorectal adenoma and carcinoma cell lines by the cyclooxygenase-2-selective non-steroidal anti-inflammatory drug NS-398. Int J Cancer, 2000, 86(4): 553-560.
[3]. Mack Strong VE, Mackrell PJ, Concannon EM, et al. NS-398 treatment after trauma modifies NF-kappaB activation and improves survival. J Surg Res, 2001, 98(1): 40-46.
| Cas No. | 123653-11-2 | SDF | |
| 别名 | 抑制剂 | ||
| 化学名 | N-(2-(cyclohexyloxy)-4-nitrophenyl)methanesulfonamide | ||
| Canonical SMILES | O=S(NC(C(OC1CCCCC1)=C2)=CC=C2[N+]([O-])=O)(C)=O | ||
| 分子式 | C13H18N2O5S | 分子量 | 314.36 |
| 溶解度 | ≥ 31.4mg/mL in DMSO | 储存条件 | Store at -20℃ |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。