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/ Nimesulide/尼美舒利

Nimesulide/尼美舒利 {[allProObj[0].p_purity_real_show]}

货号：A370794 同义名： R805

Nimesulide是发酵食品和酒精饮料中的天然副产物，被归类为 2A 类可能的人类致癌物。它具有抑制细菌、原生动物和植物组织生长的能力，是食品安全研究的重要目标分子。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Nimesulide/尼美舒利 化学结构 CAS号：51803-78-2
Nimesulide/尼美舒利 化学结构
CAS号：51803-78-2
Nimesulide/尼美舒利 3D分子结构
CAS号：51803-78-2
Nimesulide/尼美舒利 化学结构 CAS号：51803-78-2
Nimesulide/尼美舒利 3D分子结构 CAS号：51803-78-2
规格 价格 会员价 库存 数量
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Nimesulide/尼美舒利 纯度/质量文件 产品仅供科研

货号：A370794 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

Nimesulide/尼美舒利 生物活性

靶点

  • COX-2

    COX-2, IC50:26 μM
描述 Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties[3]. Nimesulide, but not indomethacin, reduced the fever induced by MIP-1alpha, PGF(2alpha), CRF or ET-1. Plasma TNF-alpha levels in LPS-treated rats were also reduced by nimesulide[4]. Nimesulide (10 µM) effectively decreases VEGF in endometrium cancer cells, and shows no effect on that in normal cells. Nimesulide (10 and 50 µM) dramatically decreases MCP-1 levels in normal cell, and such an effect is also observed with 10 µM in cancer cells. In addition, Nimesulide (50 µM) potently affects IL-8 level in normal cells, but causes no changes in cancer cells[5].

Nimesulide/尼美舒利 细胞实验

Cell Line
Concentration Treated Time Description References
Murine aortic smooth muscle cells 0.1–1 µM 48 hours Nimesulide completely reversed the antimitogenic effect of APOE J Clin Invest. 2004 Feb;113(4):609-18.
Mouse tracheal smooth muscle cells 1 μM 10 minutes To investigate the effect of nimesulide on SLIGRL-NH2-induced tracheal smooth muscle relaxation and PGE2 release, results showed that nimesulide significantly attenuated SLIGRL-NH2-induced relaxation and PGE2 release. Br J Pharmacol. 2001 Jan;132(1):93-100.

Nimesulide/尼美舒利 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
LDL receptor knockout mice High-fat diet-induced atherosclerosis model Drinking water administration 40 mg/liter 18 weeks To evaluate the effect of nimesulide on atherosclerosis. Results showed that nimesulide inhibited COX-2 activity without affecting platelet function and did not significantly alter the progression of atherosclerosis. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3358-63
Mice KrasG12D/+;Trp53−/− non-small-cell lung cancer graft model Intraperitoneal injection 5 mg/kg Single dose To evaluate the therapeutic effect of Nimesulide in combination with Bortezomib on Kras-driven non-small-cell lung cancer, results showed enhanced apoptotic response in tumor cells. J Exp Med. 2018 Dec 3;215(12):3115-3135
Mice Adult mouse brain neurogenesis model Intraperitoneal injection 10 mg/kg Once daily for 5 days Evaluate the effects of nimesulide on brain neurogenesis, results showed significant inhibition of progenitor cell proliferation in the SVZ Br J Pharmacol. 2010 Mar;159(5):1118-25
Mice EC-AMPK transgenic mice Oral gavage 25 mg/kg/day Once daily for 4 weeks Nimesulide significantly ameliorated arterial inflammation, steatohepatitis and hyperlipidaemia in EC-AMPK mice, without altering their blood pressure or clotting. Br J Pharmacol. 2014 Jan;171(2):498-508

Nimesulide/尼美舒利 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
NCT02466581 Rheumatoid Arthritis Phase 4 Recruiting December 2021 Sweden ... 展开 >> Karolinska Institutet Recruiting Stockholm, Sweden, 171 76 Contact: Ronald van Vollenhoven, MD, prof    +46(8)51776077    ronald.van.vollenhoven@ki.se    Contact: Monica Ryden Aulin, PhD    +46(8)51771110    monica.ryden.aulin@ki.se 收起 <<
NCT02563756 Knee Osteoarthritis Not Applicable Recruiting September 2022 Sweden ... 展开 >> Karolinska University Hospital Recruiting Stockholm, Sweden Contact: Carl Aulin, MD       carl.aulin@karolinska.se    Contact: Nicolas Martinez, MD    +46709900089    nicolas.martinez-carranza@karolinska.se 收起 <<
NCT03104985 - Completed - -

Nimesulide/尼美舒利 参考文献

[1]Rainsford KD; Members of the Consensus Report Group on Nimesulide. Nimesulide -- a multifactorial approach to inflammation and pain: scientific and clinical consensus. Curr Med Res Opin. 2006 Jun;22(6):1161-70.

[2]Bernareggi A. Clinical pharmacokinetics of nimesulide. Clin Pharmacokinet. 1998 Oct;35(4):247-74.

[3]Vago T, Bevilacqua M, Norbiato G. Effect of nimesulide action time dependence on selectivity towards prostaglandin G/H synthase/cyclooxygenase activity. Arzneimittelforschung.1995;45(10):1096-1098

[4]Werner MF, Souza GE, Zampronio AR. Nimesulide-induced antipyresis in rats involves both cyclooxygenase-dependent and independent mechanisms. Eur J Pharmacol. 2006;543(1-3):181-189

[5]Genç S, Attar E, Gürdöl F, Kendigelen S, Bilir A, Serdaroğlu H. The effect of COX-2 inhibitor, nimesulide, on angiogenetic factors in primary endometrial carcinoma cell culture. Clin Exp Med. 2007;7(1):6-10

Nimesulide/尼美舒利 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.22mL

3.24mL

1.62mL

32.43mL

6.49mL

3.24mL

Nimesulide/尼美舒利 技术信息

CAS号51803-78-2
分子式C13H12N2O5S
分子量 308.31
SMILES Code CS(=O)(NC1=CC=C([N+]([O-])=O)C=C1OC2=CC=CC=C2)=O
MDL No. MFCD00079470
别名 R805
运输蓝冰
InChI Key HYWYRSMBCFDLJT-UHFFFAOYSA-N
Pubchem ID 4495
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: 105 mg/mL(340.57 mM)，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

请根据您的动物给药指南选择适当的溶解方案。
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
方案 一
方案 二

Tags: Nimesulide | 51803-78-2 | R805 | R 805 | R-805 | COX Inhibitor | Immunology/Inflammation | COX | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Nimesulide/尼美舒利 纯度/质量文件 | Nimesulide/尼美舒利 亚型比较 | Nimesulide/尼美舒利 生物活性 | Nimesulide/尼美舒利 临床数据 | Nimesulide/尼美舒利 参考文献 | Nimesulide/尼美舒利 实验方案 | Nimesulide/尼美舒利 技术信息

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