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Parecoxib/帕瑞昔布 {[allProObj[0].p_purity_real_show]}

货号:A203658 同义名: Vorth-P; Valus-P

Parecoxib是一种强效且选择性的COX2抑制剂,可抑制前列腺素(PG) 的合成,缓解术后急性疼痛和骨关节炎、类风湿关节炎等慢性炎症症状。

Parecoxib/帕瑞昔布 化学结构 CAS号:198470-84-7
Parecoxib/帕瑞昔布 化学结构
CAS号:198470-84-7
Parecoxib/帕瑞昔布 3D分子结构
CAS号:198470-84-7
Parecoxib/帕瑞昔布 化学结构 CAS号:198470-84-7
Parecoxib/帕瑞昔布 3D分子结构 CAS号:198470-84-7
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Parecoxib/帕瑞昔布 纯度/质量文件 产品仅供科研

货号:A203658 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Parecoxib/帕瑞昔布 生物活性

靶点
  • COX-2

描述 Parecoxib is a potent and selective COX-2 inhibitor. Parecoxib ameliorated postischemic mitochondria-mediated neuronal apoptosis induced by focal cerebral ischemia in rats and this neuroprotective potential is involved in phosphorylation of Akt and GSK-3β[3]. The prodrug Parecoxib as well as its active metabolite val have a specific affinity to the cannabinoid (CB) receptor measured in CB1-expressing HEK 293 cells and rat brain tissue. The analgesic effects of par and its metabolite val in Wistar rats may be at least partially mediated by a direct interaction with the CB1 receptors[4]. The COX-2 inhibitor parecoxib exerts its analgesic effect on surgical pain through the inhibition of neuronal ERK activation in the spinal cord. COX-2 inhibitor delivery prior to surgery has more potent analgesic effects[5]. Despite the absence of clinical adverse effects, parecoxib can impair anastomotic and abdominal wound healing on a histopathological level[6].

Parecoxib/帕瑞昔布 细胞实验

Cell Line
Concentration Treated Time Description References
AC2F rat liver cells 5, 10, 20, 40, 80 µM 12 hours or 48 hours To evaluate the cytotoxicity of parecoxib to Ac2F cells Biomol Ther (Seoul). 2021 Sep 1;29(5):519-526
Human colorectal cancer DLD-1 cells 3 µM 48 hours Parecoxib enhances resveratrol's ability to inhibit DLD-1 cell viability and increases apoptosis by inhibiting TXNDC5 and Akt phosphorylation. Nutrients. 2024 Sep 6;16(17):3020
SW480 cells 3 µM 48 hours To evaluate the inhibitory effect of parecoxib combined with 5-FU on the migration and invasion of SW480 cells. The results showed that the combination of parecoxib and 5-FU significantly inhibited cell migration and invasion. Biomedicines. 2024 Jul 9;12(7):1526
DLD-1 cells 3 µM 48 hours To evaluate the inhibitory effect of parecoxib combined with 5-FU on the migration and invasion of DLD-1 cells. The results showed that the combination of parecoxib and 5-FU significantly inhibited cell migration and invasion. Biomedicines. 2024 Jul 9;12(7):1526
3T3-L1 murine preadipocytes 15, 30, 60 µM 8 days To evaluate the effect of parecoxib on adipocyte differentiation Biomol Ther (Seoul). 2021 Sep 1;29(5):519-526

Parecoxib/帕瑞昔布 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Pulmonary ischemia-reperfusion injury model Intraperitoneal injection 10 mg/kg Once daily for 5 consecutive days Parecoxib sodium pretreatment alleviates pulmonary ischemia-reperfusion injury by inhibiting the ERK/NF-κB pathway and further activating the HIF-1α pathway. Immun Inflamm Dis. 2022 Sep;10(9):e684
Sprague-Dawley rats Ischemia reperfusion-induced intestinal injury model Intraperitoneal injection 10 or 20 mg/kg Once daily for 5 consecutive days Parecoxib sodium pre-treatment significantly attenuated ischemia reperfusion-induced oxidative stress, inflammatory responses, and apoptosis, and increased the survival rate of rats. Mol Med Rep. 2021 Nov;24(5):776

Parecoxib/帕瑞昔布 参考文献

[1]Ye Z, Wang N,et al. Delayed administration of parecoxib, a specific COX-2 inhibitor, attenuated postischemic neuronal apoptosis by phosphorylation Akt and GSK-3β. Neurochem Res. 2012 Feb;37(2):321-9.

[2]Meunier A, Aspenberg P. Parecoxib impairs early metaphyseal bone healing in rats. Arch Orthop Trauma Surg. 2006 Sep;126(7):433-6.

[3]Ye Z, Wang N, Xia P, Wang E, Yuan Y, Guo Q. Delayed administration of parecoxib, a specific COX-2 inhibitor, attenuated postischemic neuronal apoptosis by phosphorylation Akt and GSK-3β. Neurochem Res. 2012;37(2):321-329

[4]Schröder H, Höllt V, Becker A. Parecoxib and its metabolite valdecoxib directly interact with cannabinoid binding sites in CB1-expressing HEK 293 cells and rat brain tissue. Neurochem Int. 2011;58(1):9-13

[5]Guo YJ, Shi XD, Fu D, Yang Y, Wang YP, Dai RP. Analgesic effects of the COX-2 inhibitor parecoxib on surgical pain through suppression of spinal ERK signaling. Exp Ther Med. 2013;6(1):275-279

[6]Martinou E, Drakopoulou S, Aravidou E, et al. Parecoxib's effects on anastomotic and abdominal wound healing: a randomized Controlled trial. J Surg Res. 2018;223:165-173

Parecoxib/帕瑞昔布 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.00mL

5.40mL

2.70mL

Parecoxib/帕瑞昔布 技术信息

CAS号198470-84-7
分子式C19H18N2O4S
分子量 370.42
SMILES Code CCC(NS(=O)(C1=CC=C(C2=C(C)ON=C2C3=CC=CC=C3)C=C1)=O)=O
MDL No. MFCD25976408
别名 Vorth-P; Valus-P; SC 69124
运输蓝冰
InChI Key TZRHLKRLEZJVIJ-UHFFFAOYSA-N
Pubchem ID 119828
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

DMSO: 50 mg/mL(134.98 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
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