SML2928
Lumiracoxib
≥98% (HPLC)
别名:
2-[(2-Chloro-6-fluorophenyl)amino]-5-methyl-benzeneacetic acid, 5-Methyl-2-(2′-chloro-6′-fluoroanilino)phenylacetic acid, CGS 35189, CGS-35189, CGS35189, COX 189, COX-189, COX189, LMX, Non-steroidal anti-inflammatory drug
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
ClC1=CC=CC(F)=C1NC2=CC=C(C)C=C2CC(O)=O
InChI
1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20)
InChI key
KHPKQFYUPIUARC-UHFFFAOYSA-N
相关类别
生化/生理作用
Lumiracoxib (COX189) is an orally active, potent and selective cyclooxygenase-2 inhibitor (Ki = 60 nM/COX-2 vs. 3.2 μM/COX-1) that inhibits COX-2-mediated PGE2 production in human whole blood (IC50 = 130 nM; stimulation = 50 μM A23187), but not COX-1-dependent TxB2 production (IC50 = 67 μM; stimulation = 10 μg/mL LPS). Lumiracoxib shows in vivo anti-inflammatory efficacy against carrageenan-induced paw oedema (ED30 = 0.35 mg/kg p.o.), CFA-induced hyperalgesia (ED30 = 5.1 mg/kg p.o.), as well as adjuvant-induced arthritis (ED50 = 3 mg/kg/day p.o.) in rats in vivo.
Orally active, potent and selective cyclooxygenase-2 (COX-2) inhibitor with anti-inflammatory efficacy in vivo.
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Amanda J Morgan et al.
ACS chemical neuroscience, 9(7), 1552-1559 (2018-05-04)
Cyclooxygenase-2 (COX-2) catalyzes the formation of prostaglandins, which are involved in immune regulation, vascular function, and synaptic signaling. COX-2 also inactivates the endogenous cannabinoid (eCB) 2-arachidonoylglycerol (2-AG) via oxygenation of its arachidonic acid backbone to form a variety of prostaglandin
Ronald Esser et al.
British journal of pharmacology, 144(4), 538-550 (2005-01-19)
1. This manuscript presents the preclinical profile of lumiracoxib, a novel cyclooxygenase-2 (COX-2) selective inhibitor. 2. Lumiracoxib inhibited purified COX-1 and COX-2 with K(i) values of 3 and 0.06 microM, respectively. In cellular assays, lumiracoxib had an IC(50) of 0.14
Amanda Morgan et al.
Neurobiology of stress, 11, 100190-100190 (2019-08-31)
Chronic stress increases the probability of receiving an anxiety, depression, or chronic illness diagnosis. Pharmacological interventions that reduce the behavioral and physiological effects of chronic stress in animal models may represent novel approaches for the treatment of stress-related psychiatric disorders.
Christina Brummer et al.
Cancer letters, 442, 453-463 (2018-11-28)
Tumors, including melanomas, frequently show an accelerated glucose metabolism. Mutations in the v-Raf murine sarcoma viral oncogene homolog B (BRAF), detected in about 50% of all melanomas, result in further enhancement of glycolysis. Therefore anti-metabolic substances might enhance the impact
Alyson Fox et al.
Pain, 107(1-2), 33-40 (2004-01-13)
Chronic pain resulting from metastatic bone cancer remains poorly understood and resistant to treatment. Here we have examined the effect of the novel COX-2 enzyme inhibitor lumiracoxib in a model of bone cancer pain in the rat. Lumiracoxib was administered
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