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Merck
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Key Documents

SML2928

Sigma-Aldrich

Lumiracoxib

≥98% (HPLC)

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C15H13ClFNO2
CAS號碼:
分子量::
293.72
MDL號碼:
分類程式碼代碼:
51111800
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

SMILES 字串

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 密鑰

KHPKQFYUPIUARC-UHFFFAOYSA-N

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.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Acute Tox. 4 Oral

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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.
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
Weijie Jiao et al.
Drug testing and analysis, 12(6), 827-835 (2020-02-12)
Lumiracoxib is a selective cyclooxygenase-2 inhibitor, which has been reported to cause rare but severe liver injury. Considering that lumiracoxib has a carboxylic group in the molecule, glucuronidation to form acylglucuronide would be one of the possible mechanisms of lumiracoxib-induced
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
S S Ahmed et al.
Toxicology and applied pharmacology, 369, 39-48 (2019-02-16)
The occurrence of drug hypersensitivity reactions (DHRs) following administration of low molecular weight (LMW) drugs is an important health concern. However, in vivo animal models which could be used as tools for the prediction of DHRs are lacking. As a

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