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Piroxicam/吡罗昔康 {[allProObj[0].p_purity_real_show]}

货号:A265438 同义名: CP-16171; NSC 666076

Piroxicam是一种选择性COX1抑制剂,具有抗炎活性,对人单核细胞 COX-1 和 COX-2 的 IC50 值分别为 47 和 25 μM。

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+
Piroxicam/吡罗昔康 化学结构 CAS号:36322-90-4
Piroxicam/吡罗昔康 化学结构
CAS号:36322-90-4
Piroxicam/吡罗昔康 3D分子结构
CAS号:36322-90-4
Piroxicam/吡罗昔康 化学结构 CAS号:36322-90-4
Piroxicam/吡罗昔康 3D分子结构 CAS号:36322-90-4
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Piroxicam/吡罗昔康 纯度/质量文件 产品仅供科研

货号:A265438 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。

Piroxicam/吡罗昔康 生物活性

靶点
  • COX

描述 Piroxicam is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively[3]. Piroxicam (0.3 mg/kg qd 24-h p.o.) reduces tumor volume in 12 of 18 dogs, and such and effect is via induction of apoptosis and reduction in urine basic fibroblast growth factor concentration[4]. Piroxicam (167, 333, 500 μM) decreases cell population of T24 and the 5637 cells. Piroxicam (500 μM) also reduces the cell viability of T24 and 5637 cell, and is significantly effective when combined with 0.05 μM carboplatin. The combination also inhibits Ki-67 expression in booth cells. In vitro combination of carboplatin and piroxicam produced a more potent antiproliferative effect when compared to single drugs[5].

Piroxicam/吡罗昔康 细胞实验

Cell Line
Concentration Treated Time Description References
Neuro 2A (N-2A) neuroblastoma cells 5 mM 24 hours To evaluate the protective effects of piroxicam against MPP+ toxicity, results showed piroxicam significantly increased cell viability at 5 mM (from 15±2% to 89±4%) Neurochem Res. 2009 Feb;34(2):304-10
A-172 cells 3, 14, 30 µM 72 hours To evaluate the effect of piroxicam on A-172 cells, results showed a protective effect on PBMCs and reduced the fraction of cells in the G2/M phase. Sci Rep. 2022 Nov 17;12(1):19806
U-87 MG cells 3, 14, 30 µM 72 hours To evaluate the effect of piroxicam on U-87 MG cells, results showed a protective effect on PBMCs. Sci Rep. 2022 Nov 17;12(1):19806
Peripheral blood mononuclear cells (PBMCs) 3, 14, 30 µM 72 hours To evaluate the effect of piroxicam on PBMC proliferation, results showed no adverse effect on proliferation. Sci Rep. 2022 Nov 17;12(1):19806
Full thickness rat skin 0.5% w/w 8 hours Assess the permeability of piroxicam through rat skin, with formula F3 showing significantly higher steady-state flux. Int J Nanomedicine. 2010 Nov 4;5:915-24
Cellulose acetate membrane 0.5% w/w 8 hours Evaluate the release rate of piroxicam from nanocream, showing that formula F3 released 100% of the drug within 8 hours. Int J Nanomedicine. 2010 Nov 4;5:915-24

Piroxicam/吡罗昔康 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Dogs Malignant Mesothelioma Oral 0.3 mg/kg Daily (dogs) and every other day (cats), for 4 months To evaluate the efficacy of piroxicam combined with platinum-based chemotherapy for malignant mesothelioma. Results showed that the combination effectively controlled malignant effusion, with one dog remaining in remission after 3 years, while another dog and a cat died due to disease progression after 8 and 6 months, respectively. J Exp Clin Cancer Res. 2008 May 19;27(1):6
Sprague-Dawley rats Carrageenan-induced hind paw edema model Topical application 0.5% w/w Single dose, lasting 6 hours Evaluate the anti-inflammatory and analgesic effects of piroxicam nanocream, with formula F3 showing the highest effects. Int J Nanomedicine. 2010 Nov 4;5:915-24
Male albino mice Piroxicam-induced liver and kidney injury model Administered through drinking water 0.8 mg/kg Daily administration for 6 weeks To investigate the side effects of piroxicam on liver and kidney functions and evaluate the mitigating effects of selenium-enriched probiotics. Results showed that piroxicam significantly increased levels of urea, creatinine, bilirubin, SGOT, SGPT, and ALP, while selenium-enriched probiotics (especially BSe50/20/1) significantly improved these parameters. Inflammopharmacology. 2022 Dec;30(6):2097-2106
Charles Foster rats Middle cerebral artery occlusion (MCAO) model Intraperitoneal injection 10 mg/kg Single dose 30 minutes prior to MCAO To investigate the effects of Piroxicam on 5-hydroxytryptamine (5-HT) levels and its probable GABA agonism following cerebral ischemia. Results showed that Piroxicam pretreatment significantly decreased extracellular 5-HT release in the ischemic cerebral cortex and striatum, suggesting that Piroxicam may reduce 5-HT release through GABA agonism. Neural Regen Res. 2015 Sep;10(9):1418-20
IL-10-deficient mice Piroxicam-accelerated colitis model Standard chow diet 150 mg/kg 10 days Piroxicam-induced colitis was associated with significant alterations of the intestinal barrier function, including increased permeability, changes in inflammation-related bioactive lipid mediators, and alterations in mucosal CD4+T lymphocyte subsets. Int J Mol Sci. 2021 Jul 9;22(14):7387
C57/BL6 male mice MPTP-induced Parkinson's disease model Intraperitoneal injection 20 mg/kg 3-day pretreatment, continued until the end of the study To evaluate the protective effects of piroxicam against MPTP-induced SNc dopaminergic neuron degeneration and loss of locomotive function, results showed piroxicam significantly reversed the losses in SNc tyrosine hydroxylase protein expression, SNc DA concentration and associated anomaly in ambulatory locomotor activity Neurochem Res. 2009 Feb;34(2):304-10
T-cell receptor alpha chain-deficient mice Model of synchronized colitis Oral 200 ppm w/w 14 consecutive days Piroxicam induced a time-prescribed colitis in the proximal colon and cecum of TCR α-deficient mice. Piroxicam administration induced epithelial hyperplasia, goblet cell loss, and leukocyte infiltration with occasional ulceration. Inflammation was multifocal segmental, with areas of tissue damage in between healthy tissue. In addition, variability in the severity of inflammation was observed among replicate animals and treatments, and the administration of dexamethasone only partially ameliorated inflammation in the proximal colon. Animal Model Exp Med. 2024 Aug;7(4):533-543
Wistar albino male rats Piroxicam-induced gastric ulcer and hepato-renal toxicity model Intraperitoneal injection 7 mg/kg Once daily for 28 days To investigate the protective effects of CoQ10 against piroxicam-induced oxidative injury and apoptotic pathways. Results showed that piroxicam caused gastric ulceration and hepato-renal damage, which were significantly mitigated by CoQ10. Biomed Pharmacother. 2020 Oct;130:110627

Piroxicam/吡罗昔康 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
NCT03038321 Non-Muscle-invasive Bladder Ca... 展开 >>ncer (NMIBC) Bacillus Calmette-Guerin (BCG) Cystitis Intra-vesical Instillation 收起 << Phase 4 Active, not recruiting December 2019 Egypt ... 展开 >> Urology and Nephrology Center Mansoura, Aldakahlia, Egypt, 35516 收起 <<
NCT02457325 Impacted Third Molar Tooth ... 展开 >> Adverse Reaction to Other Local Anesthetics 收起 << Phase 4 Completed - -
NCT02160236 Postoperative Pain Phase 4 Unknown February 2015 Turkey ... 展开 >> Erciyes Universty Hospital Recruiting Kayseri, Turkey, 38039 Contact: nazife küçük, resident    +905072317446    nzfkucuk@hotmail.com 收起 <<

Piroxicam/吡罗昔康 参考文献

[1]Vartiainen N, Huang CY, et al. Piroxicam and NS-398 rescue neurones from hypoxia/reoxygenation damage by a mechanism independent of cyclo-oxygenase inhibition. J Neurochem. 2001 Jan;76(2):480-9.

[2]Rigas B, Tsioulias GJ, et al. The effect of bile acids and piroxicam on MHC antigen expression in rat colonocytes during colon cancer development. Immunology. 1994 Oct;83(2):319-23.

[3]Kato M, Nishida S, Kitasato H, Sakata N, Kawai S. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of non-steroidal anti-inflammatory drugs: investigation using human peripheral monocytes. J Pharm Pharmacol. 2001;53(12):1679-1685

[4]Mohammed SI, Bennett PF, Craig BA, et al. Effects of the cyclooxygenase inhibitor, piroxicam, on tumor response, apoptosis, and angiogenesis in a canine model of human invasive urinary bladder cancer. Cancer Res. 2002;62(2):356-358

[5]Silva J, Arantes-Rodrigues R, Pinto-Leite R, et al. Synergistic Effect of Carboplatin and Piroxicam on Two Bladder Cancer Cell Lines. Anticancer Res. 2017;37(4):1737-1745

Piroxicam/吡罗昔康 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.18mL

6.04mL

3.02mL

Piroxicam/吡罗昔康 技术信息

CAS号36322-90-4
分子式C15H13N3O4S
分子量 331.35
SMILES Code O=C(C1=C(O)C2=CC=CC=C2S(N1C)(=O)=O)NC3=NC=CC=C3
MDL No. MFCD00057317
别名 CP-16171; NSC 666076
运输蓝冰
InChI Key QYSPLQLAKJAUJT-UHFFFAOYSA-N
Pubchem ID 54676228
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: 50 mg/mL(150.9 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

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
方案 三
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