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阿西美辛 /Acemetacin 98%

货号:A374323 同义名: TVX 1322 Ambeed 开学季,买赠积分,赢豪礼

Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.

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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+
Acemetacin 化学结构 CAS号:53164-05-9
Acemetacin 化学结构
CAS号:53164-05-9
Acemetacin 3D分子结构
CAS号:53164-05-9
Acemetacin 化学结构 CAS号:53164-05-9
Acemetacin 3D分子结构 CAS号:53164-05-9
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Acemetacin 纯度/质量文件 产品仅供科研

货号:A374323 标准纯度: 98%
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 99%
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%
Rofecoxib ++++

COX-2, IC50: 18 nM

98%
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

98%
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。

Acemetacin 生物活性

靶点
  • COX

描述 Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor. With purified COX-1(cyclo-oxygenase), inhibition was absent with nimesulide, weak with acemetacin (inhibitory concentration of 50% [IC50 ] 85 m̈mol/L), and potent with indomethacin (IC50 0.6 m̈mol/L). Acemetacin did not inhibit sheep COX-2 and only weakly inhibited COX-1[3]. Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical trials. Equimolar doses of acemetacin or indomethacin were administered orally. The antihyperalgesic and antiinflammatory effects were also similar for both indomethacin and acemetacin[4]. The increased gastric and intestinal tolerability of acemetacin may be related to the lack of induction of leukocyte-endothelial adherence. This may be attributable to the reduced ability of acemetacin to elevate leukotriene-B(4) synthesis and TNF-alpha expression, compared to indomethacin, despite the fact that acemetacin is rapidly bioconverted to indomethacin after its absorption[5].

Acemetacin 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
NCT01759355 - Active, not recruiting May 2019 United States, North Carolina ... 展开 >> University of North Carolina-Chapel Hill Chapel Hill, North Carolina, United States, 27599 收起 <<

Acemetacin 参考文献

[1]Chavez-Pina AE, McKnight W, et al. Mechanisms underlying the anti-inflammatory activity and gastric safety of acemetacin. Br J Pharmacol. 2007 Nov;152(6):930-8.

[2]Tavares IA, Bennett A. Acemetacin and indomethacin: differential inhibition of constitutive and inducible cyclo-oxygenases in human gastric mucosa and leucocytes. Int J Tissue React. 1993;15(2):49-53.

[3]Tavares IA, Bennett A. Non-steroidal anti-inflammatory drugs that cause relatively little gastric damage. J Gastroenterol Hepatol. 1998;13(S3):S190-S192

[4]Gil-Flores M, Ortiz MI, Castañeda-Hernández G, Chávez-Piña AE. Acemetacin antinociceptive mechanism is not related to NO or K+ channel pathways. Methods Find Exp Clin Pharmacol. 2010;32(2):101-105

[5]Chávez-Piña AE, Vong L, McKnight W, et al. Lack of effects of acemetacin on signalling pathways for leukocyte adherence may explain its gastrointestinal safety. Br J Pharmacol. 2008;155(6):857-864

Acemetacin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.02mL

2.40mL

1.20mL

24.05mL

4.81mL

2.40mL

Acemetacin 技术信息

CAS号53164-05-9
分子式C21H18ClNO6
分子量 415.824
别名 TVX 1322
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 120 mg/mL(288.58 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
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