产品说明书

NS-398

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Chemical Structure| 123653-11-2 同义名 : N-(2-cyclohexyloxy-4-nitrophenyl)methane sulfonamide
CAS号 : 123653-11-2
货号 : A113156
分子式 : C13H18N2O5S
纯度 : 98%
分子量 : 314.357
MDL号 : MFCD00882995
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
生物活性
靶点

  • COX-2

    COX-2, IC50:3.8 μM
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].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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
临床研究
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 <<
实验方案
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
参考文献

[1]Sun Y, Yu J, et al. Inhibition of cyclooxygenase-2 by NS398 attenuates noise-induced hearing loss in mice. Sci Rep. 2016 Mar 3;6:22573.

[2]Meyer-Siegler K. COX-2 specific inhibitor, NS-398, increases macrophage migration inhibitory factor expression and induces neuroendocrine differentiation in C4-2b prostate cancer cells. Mol Med. 2001 Dec;7(12):850-60.

[3]Kava MS, Blue DR Jr, Vimont RL, Clarke DE, Ford AP. Alpha1L-adrenoceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man. Br J Pharmacol. 1998 Apr;123(7):1359-66. doi: 10.1038/sj.bjp.0701748. PMID: 9579731; PMCID: PMC1565303.

[4]Futaki N, Takahashi S, Yokoyama M, Arai I, Higuchi S, Otomo S. 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. doi: 10.1016/0090-6980(94)90074-4. PMID: 8140262.

[5]Shen W, Li Y, Tang Y, Cummins J, Huard J. NS-398, a cyclooxygenase-2-specific inhibitor, delays skeletal muscle healing by decreasing regeneration and promoting fibrosis. Am J Pathol. 2005 Oct;167(4):1105-17. doi: 10.1016/S0002-9440(10)61199-6. PMID: 16192645; PMCID: PMC1603662.

[6] Meyer-Siegler K. COX-2 specific inhibitor, NS-398, increases macrophage migration inhibitory factor expression and induces neuroendocrine differentiation in C4-2b prostate cancer cells. Mol Med. 2001 Dec;7(12):850-60. PMID: 11876163; PMCID: PMC1950011.

[7]Sun Y, Yu J, Lin X, Tang W. Inhibition of cyclooxygenase-2 by NS398 attenuates noise-induced hearing loss in mice. Sci Rep. 2016 Mar 3;6:22573. doi: 10.1038/srep22573. PMID: 26934825; PMCID: PMC4776277.