Parecoxib
(Synonyms: 帕瑞昔布; SC 69124) 目录号 : GC36852
A prodrug form of valdecoxib
Cas No.:198470-84-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Parecoxib is a prodrug form of the COX-2 inhibitor valdecoxib .1 It is converted to valdecoxib by human liver microsomes in vitro and in vivo in rats, dogs, and cynomolgous monkeys. Parecoxib is also a cannabinoid (CB) receptor 1 agonist with an EC50 value of 2.4 ?M in HEK293 cells.2 It reduces hyperalgesia in a rat model of carrageenan-induced foot pad edema (ED50 = 5 mg/kg) and decreases inflammation in a rat model of M. butyricum-induced arthritis (ED50 = 0.08 mg/kg).1
1.Talley, J.J., Bertenshaw, S.R., Brown, D.L., et al.N-[[(5-methyl-3-phenylisoxazol-4-yl)-phenyl]sulfonyl]propanamide, sodium salt, parecoxib sodium: A potent and selective inhibitor of COX-2 for parenteral administrationJ. Med. Chem.43(9)1661-1663(2000) 2.Schr?der, H., H?llt, V., and Becker, A.Parecoxib and its metabolite valdecoxib directly interact with cannabinoid binding sites in CB1-expressing HEK 293 cells and rat brain tissueNeurochem. Int.58(1)9-13(2011)
| Cas No. | 198470-84-7 | SDF | |
| 别名 | 帕瑞昔布; SC 69124 | ||
| Canonical SMILES | CCC(NS(=O)(C1=CC=C(C2=C(C)ON=C2C3=CC=CC=C3)C=C1)=O)=O | ||
| 分子式 | C19H18N2O4S | 分子量 | 370.42 |
| 溶解度 | DMSO: ≥ 50 mg/mL (134.98 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL |
| 10 mM | 0.27 mL | 1.3498 mL | 2.6996 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Parecoxib ameliorates renal toxicity and injury in sepsis-induced mouse model and LPS-induced HK-2 cells
Drug Dev Res 2022 May;83(3):659-668.PMID:34813666DOI:10.1002/ddr.21897.
Parecoxib is a selective COX-2-specific inhibitor, which has been demonstrated to inhibit sepsis-induced systemic inflammation, but its role in sepsis-induced acute kidney injury has not been studied. This study was designed to investigate the effects of Parecoxib on sepsis-induced acute kidney injury. In this study, the mice sepsis model was established using an internationally recognized cecal ligation and puncture (CLP). Hematoxylin-eosin staining was performed to examine kidney injury. Biochemical kit was used to detect the expression of BUN and Cre in serum, and ELISA was used to detect the expression of inflammatory factors in renal tissue. Tunel staining was used to detect tissue apoptosis. Furthermore, CCK-8 assay was used to detect the cell viability of HK-2 cells and RT-qPCR was used to detect the expression of LPS-induced inflammatory factors in HK-2 cells.TUNEL staining was used to detect the level of cell apoptosis. Finally, the expressions of COX-2, p-NF-kB P65, p-IKKβ, NF-kB P65, IKKβ, Kim1, NGAL, iNOS, VEGF, VEGFR2, CD31 and apoptosis-related proteins in renal tissues and HK-2 cells were detected by Western blot. We discovered that Parecoxib could alleviate renal pathological changes, reduce renal function injury, and inhibit renal pathology to inhibit the release of inflammatory factors in renal tissue. Parecoxib inhibited sepsis induced microvascular damage and apoptosis in renal tissue. Parecoxib reduced the inflammation and apoptosis of renal tubular epithelial cells induced by LPS. Our data suggest that Parecoxib ameliorates sepsis-induced kidney injury, and may have potential as a novel therapeutic method for treating sepsis-induced kidney injury.
Intravenous Parecoxib for Pain Relief after Orthopedic Surgery: A Systematic Review and Meta-analysis
Pain Ther 2022 Sep;11(3):771-787.PMID:35705843DOI:10.1007/s40122-022-00400-1.
Introduction: Orthopedic procedures have been associated with increased pain, making perioperative analgesia a major clinical concern. We assessed the efficacy and safety of intravenous Parecoxib administration during the perioperative period for postoperative pain relief after orthopedic surgery in adults. Methods: PubMed, Cochrane Library, EMBASE, and clinicaltrial.gov were searched from inception to 23 August 2021 without language restrictions. Randomized controlled trials comparing intravenous Parecoxib with placebo or another active treatment for acute postoperative pain in adults after orthopedic surgery were included. The primary outcomes were the pain scores and cumulative morphine consumption. The secondary outcomes included the proportion of patients requiring rescue analgesics and the incidence of adverse events. The meta-analysis followed the Preferred Reporting Items for Systematic Reviews and Meta-analyses guidelines and was registered on the International Prospective Register of Systematic Reviews Registration (PROSPERO). Results: Twenty-seven trials (n = 2840) from more than 20 countries involving six types of orthopedic surgery met the inclusion criteria. Compared with placebo, intravenous Parecoxib administration led to reductions in postoperative resting pain scores at 6, 12, 24, and 48 h [mean difference (MD) -0.87, 95% confidence interval [CI] -1.71 to -0.03; MD -0.86, 95% CI -1.26 to -0.46; MD -0.57, 95% CI -0.84 to -0.31; MD -0.40, 95% CI -0.69 to -0.11, respectively], postoperative movement pain scores at 24 and 48 h (MD -0.66, 95% CI -1.14 to -0.19; MD -0.78, 95% CI -1.16 to -0.39, respectively), cumulative morphine consumption (MD -11.30 mg, 95% CI -14.79 to -7.81 mg), and the proportion of patients requiring rescue analgesia (relative risk 0.83, 95% CI 0.77-0.89). There was no difference in the incidence of adverse events between groups. Conclusion: Low to moderate evidence indicates that Parecoxib might be an effective and safe analgesic in perioperative orthopedic settings. It relieves postoperative orthopedic pain while sparing opioid analgesic consumption without increasing the incidence of adverse events. Prospero registration: CRD42021274939.
Parecoxib for opioid-induced hyperalgesia
BMJ Support Palliat Care 2021 Jun;11(2):126-127.PMID:32601152DOI:10.1136/bmjspcare-2020-002290.
This paper describes the case report of a patient admitted to hospital with severe and complex pain and subacute bowel obstruction, who failed to respond to multiple analgesic regimens including ketamine burst and opioid rotation, and was subsequently successfully managed with a Parecoxib infusion.
Effect of Parecoxib on Postoperative Pain Management After Total Knee/Hip Arthroplasty: A Systematic Review and Meta-Analysis
Cureus 2022 Dec 9;14(12):e32339.PMID:36628043DOI:10.7759/cureus.32339.
Background: Total knee arthroplasty (TKA) or total hip arthroplasty (THA) are frequent procedures used to relieve the symptoms of hip or knee joint dysfunction, enhance disease recovery, and boost patients' quality of life. Nevertheless, postoperative pain has been a significant disadvantage since it strongly impacts patients' postoperative recovery. Parecoxib has been demonstrated to be useful in the management of postoperative pain in a variety of surgical procedures. While Parecoxib can help with postoperative pain, its analgesic and unfavourable effects in TKA/THA patients have not been well studied. Methods: A systematic search of peer-reviewed articles was conducted through the PubMed database, Google Scholar, and Cochrane library to retrieve related studies published in the English language that met inclusion and exclusion criteria. The publication date was restricted to the past 10 years (2012-2022). Results were analyzed using Review Manager software (RevMan version 5.4.1, The Cochrane Collaboration, 2020). The quality of the studies included was assessed using Jadad scores. Risk ratios (RR) standard mean difference (SMD) and 95% confidence intervals (CI) were calculated to analyze the primary and secondary endpoints. Results: Eleven randomized controlled trials covering 1911 patients who underwent TKA/THA were selected. The pooled results indicated that the Parecoxib group has lower visual analogue scale (VAS) scores than the placebo group. However, there was no significant difference in the secondary endpoint. The Jadad scores ranged from 3 to 5 and most of the studies were of high quality. Conclusion: The results of our meta-analysis indicate that Parecoxib has a better analgesic effect compared to placebo. It alleviates postoperative orthopaedic pain without raising the risk of adverse events.
Parecoxib inhibits esophageal squamous cell carcinoma progression via the PDK1-AKT pathway
Cell Mol Biol Lett 2022 Mar 19;27(1):28.PMID:35305553DOI:10.1186/s11658-022-00324-w.
Background: Parecoxib plays an important role in inhibition of human cancer. However, the effect of Parecoxib on esophageal squamous cell carcinoma (ESCC) is still not well known. The purpose of this study was to investigate the effect of Parecoxib on ESCC and its underlying mechanism. Methods: RNA-sequence analysis was performed to identify functional alterations and mechanisms. Cell cycle, proliferation, invasion, and migration were assessed using flow cytometry, CCK-8 assay, colony formation, transwell, and wound healing assays. Extracellular matrix (ECM) degradation was detected by substrate gel zymography and 3D cell culture assay. Western blotting was used to detect parecoxib-dependent mechanisms involving cell cycle, proliferation, invasion, and migration. Tumor formation in vivo was detected by mouse assay. Results: Functional experiments indicated that Parecoxib induced ESCC cell cycle arrest in G2 phase, and inhibited cell proliferation, invasion, and migration in vitro. Western blotting revealed that Parecoxib downregulated the phosphorylation levels of AKT and PDK1, as well as the expression of the mutant p53, cyclin B1, and CDK1, while upregulating p21waf1. Parecoxib inhibited matrix metalloproteinase-2 (MMP2) secretion and invadopodia formation, which were related to ECM degradation. Furthermore, we found that Parecoxib suppressed ESCC growth in heterotopic tumor models. Conclusion: Parecoxib inhibits ESCC progression, including cell cycle, proliferation, invasion, and migration, via the PDK1-AKT signaling pathway.