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Merck
모든 사진(1)

주요 문서

SML2928

Sigma-Aldrich

Lumiracoxib

≥98% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C15H13ClFNO2
CAS Number:
Molecular Weight:
293.72
MDL number:
UNSPSC 코드:
51111800
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

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

생화학적/생리학적 작용

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.

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

예방조치 성명서

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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문서 라이브러리 방문

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
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
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 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

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