货号:A113156
同义名:
N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide
NS-398是一种非甾体抗炎剂,具有镇痛和退热作用。它选择性抑制前列腺素G/H合酶2/环氧合酶2(COX-2)的活性,IC50值为3.8 μM,而对COX-1在100 μM时没有影响。


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| 产品名称 | COX ↓ ↑ | COX-1 ↓ ↑ | COX-2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Piroxicam | ✔ | 98% | |||||||||||||||||
| Salicylic acid | ✔ | 98% | |||||||||||||||||
| Phenacetin | ✔ | 98% | |||||||||||||||||
| Etodolac | ✔ | 99% | |||||||||||||||||
| Flunixin meglumine | ✔ | 98% | |||||||||||||||||
| Ibuprofen L-lysine | ✔ | 98% | |||||||||||||||||
| Nabumetone | ✔ | 98% | |||||||||||||||||
| Acemetacin | ✔ | 98% | |||||||||||||||||
| Diflunisal | ✔ | 98% | |||||||||||||||||
| Pranoprofen | ✔ | 98% | |||||||||||||||||
| Ampiroxicam | ✔ | 98% | |||||||||||||||||
| Meloxicam | ✔ | 98% | |||||||||||||||||
| Sulindac | ✔ | 98% | |||||||||||||||||
| Ketoprofen | ✔ | 98% | |||||||||||||||||
| Mefenamic Acid | ✔ | 95% | |||||||||||||||||
| Bromfenac sodium | ✔ | 98% | |||||||||||||||||
| Oxaprozin | ✔ | 99% | |||||||||||||||||
| Aspirin | ✔ | 99% | |||||||||||||||||
| Nepafenac | ✔ | 98% | |||||||||||||||||
| Zaltoprofen | ✔ | 99% | |||||||||||||||||
| Salicin | ✔ | 98% | |||||||||||||||||
| Suprofen | ✔ | 99%+ | |||||||||||||||||
| Xanthohumol | ✔ | 99% | |||||||||||||||||
| Parecoxib | ✔ | 98% | |||||||||||||||||
| Tolfenamic Acid |
+++
COX-2, IC50: 0.2 μM |
98% | |||||||||||||||||
| Etoricoxib | ✔ | 99% | |||||||||||||||||
| Niflumic Acid | ✔ | 98% | |||||||||||||||||
| Valdecoxib |
++++
COX-2, IC50: 5 nM |
99+% | |||||||||||||||||
| Ibuprofen |
+
COX-1, IC50: 13 μM |
+
COX-2, IC50: 370 μM |
98% | ||||||||||||||||
| Indomethacin |
++
COX1, IC50: 0.28 μM |
+
COX-2, IC50: 14 μM |
97% | ||||||||||||||||
| Lornoxicam |
++++
COX-1, IC50: 5 nM |
++++
COX-2, IC50: 8 nM |
98% | ||||||||||||||||
| Meclofenamic acid sodium |
++++
COX-1, IC50: 40 nM |
+++
COX-2, IC50: 50 nM |
99% | ||||||||||||||||
| Asaraldehyde | ✔ | 98% | |||||||||||||||||
| Naproxen |
+
COX-1, IC50: 8.7 μM |
+
COX-2, IC50: 5.2 μM |
98% | ||||||||||||||||
| Diclofenac Sodium Salt |
+++
COX-1, IC50: 60 nM |
+++
COX-2, IC50: 200 nM |
98% | ||||||||||||||||
| NS-398 |
++
COX-2, IC50: 3.8 μM |
95% | |||||||||||||||||
| Amfenac Sodium Hydrate |
++
COX-1, IC50: 250 nM |
+++
COX-2, IC50: 150 nM |
98%+ | ||||||||||||||||
| Nimesulide |
+
COX-2, IC50: 26 μM |
98% | |||||||||||||||||
| Lumiracoxib |
++
COX-1, Ki: 3 μM |
+++
COX-2, Ki: 60 nM |
98% | ||||||||||||||||
| Rutaecarpine | ✔ | 95% | |||||||||||||||||
| Celecoxib |
++++
COX-2, IC50: 40 nM |
98% | |||||||||||||||||
| Carprofen |
++++
canine COX2, IC50: 30 nM |
98% | |||||||||||||||||
| Ketorolac |
++
COX-1 (human), IC50: 1.23 μM |
++
COX-2 (human), IC50: 3.50 μM |
98% | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | NS-398 is a novel anti-inflammatory and analgesic agent. The COX-1 activity was completely unaffected by 100μ M NS-398, whereas the COX-2 activity was concentration-dependently inhibited with IC50 of 3.8μ M[3]. NS-398 shows the anti-inflammatory and analgesic effects with the effective dose range being 0.3∼5 mg/kg in rats[4].In vitro experiments, NS-398 inhibited the proliferation and maturation of differentiated myogenic precursor cells, which suggested a detrimental effect on skeletal muscle healing. In the NS-398-treated mice, muscle regeneration delayed at early time points after injury[5].NS-398 decreased the regeneration of injured muscle by delaying the maturation of regenerating myofibers, and promoted fibrosis by up-regulating TGF-β1 expression. NS-398 administration also reduced the inflammatory response and up-regulated myostatin expression[5]. NS-398 (10 mM) can induce apoptosis in LNCaP cells[6]. When treated with NS-398, the C4-2b cells were observed to continue to proliferate and continued to retain malignant phenotype characteristics. NS-398 treatment resulted in C4-2b cell differentiation into an unusual neuroendocrine-like cell which produced both epithelial and neuronal proteins. Moreover, this C4-2b cellular response to NS-398 was mediated by NF-kappa beta transcription factor activation[6]. Cox-2 is involved in the pathogenesis of Noise-induced hearing loss (NIHL), and pre-treatment with the Cox-2 inhibitor NS398 could inhibit Cox-2 expression during noise overstimulation attenuating noise-induced hearing loss and hair cell damage[7]. |
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| HaCaT cells | Function assay | 24 h | Inhibition of PGE2 production in human HaCaT cells after 24 hrs by RIA, IC50=0.01 μM | 15387642 | |
| HUVEC | Function assay | 18 h | Antiangiogenic activity against VEGFA-stimulated capillary differentiation in HUVEC after 18 hrs by matrigel assay | 23110475 | |
| HUVEC | Function assay | 48 h | Antiangiogenic activity against VEGFA-stimulated cell proliferation in HUVEC after 48 hrs by BrdU incorporation assay | 23110475 | |
| K562 cells | Function assay | 4 days | Inhibition of COX2 in human K562 cells assessed as blockade of AML1-ETO protein-dependent erythroid differentiation after 4 days by benzidine staining method | 19172146 | |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00172627 | - | Unknown | - | Taiwan ... 展开 >> Shih-Pei Huang Recruiting Taipei, Taiwan Contact: Shih-Pei Huang, MD 886-2-23123456 ext 3353 dtmeda5@ha.mc.ntu.edu.tw 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.91mL 3.18mL 1.59mL |
31.81mL 6.36mL 3.18mL |
|
| CAS号 | 123653-11-2 |
| 分子式 | C13H18N2O5S |
| 分子量 | 314.36 |
| SMILES Code | CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2CCCCC2)=O |
| MDL No. | MFCD00882995 |
| 别名 | N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide |
| 运输 | 蓝冰 |
| InChI Key | KTDZCOWXCWUPEO-UHFFFAOYSA-N |
| Pubchem ID | 4553 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 35 mg/mL(111.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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