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Lornoxicam
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lornoxicam图片
CAS NO:70374-39-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议
200mg电议

产品介绍
氯诺昔康 (Chlortenoxicam) 是一种 COX-1 和 COX-2 抑制剂,是一种新型非甾体抗炎药 (NSAID)。
Cas No.70374-39-9
别名氯诺昔康; Chlortenoxicam; Ro 13-9297
化学名6-chloro-4-hydroxy-2-methyl-1,1-dioxo-N-pyridin-2-ylthieno[2,3-e]thiazine-3-carboxamide
Canonical SMILESCN1C(=C(C2=C(S1(=O)=O)C=C(S2)Cl)O)C(=O)NC3=CC=CC=N3
分子式C13H10ClN3O4S2
分子量371.82
溶解度≥ 18.591mg/mL in DMSO with gentle warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: A potent COX-1 and COX-2 inhibitor with IC50 values of 5 nM and 8 nM, respectively.

Lornoxicam, a new nonsteroidal anti-inflammatory drug (NSAID) belonging to the oxicam class. By intensively inhibit COX-1 and COX-2, this drug, both in oral and parenteral formulations, shows remarkable analgesic, anti-inflammatory and antipyretic properties. [1]

In vitro: Studies on intact human cells showed that lornoxicam intensively inhibit COX-1 and COX-2 with the lowest IC50 among a large panel of NSAIDs tested. Similar findings were obtained in the whole blood for COX-1/-2. In addition lornoxicam suppressed NO formation in a dose-dependently manner with an IC50 of 65 μM. [2]

In vivo: In vivo studies found that Lornoxicam was as effective as comparative NSAIDs and that 8 mg Lornoxicam was more effective than 10 mg morphine as a pain-reliever after oral surgery. Orally administration of lornoxicam at 16-24 mg daily was more effective than tramadol at 300 mg daily in pain-alleviating after knee surgery. Compared to naproxen, Lornoxicam showed higher therapeutic potency and lower gastrointestinal toxicity. This was probably due to the short half-life of lornoxicam as compared to the other oxicams. [3]

Clinical trials: A clinical study was performed to assess the efficacy and tolerability of intravenous lornoxicam in Indian patients with postoperative pain or other acute painful traumatic conditions. Patients were treated for 3 days with intravenous lornoxicam at a dosage of 8 mg twice or three times daily. Study demonstrated that intravenous lornoxicam is a powerful NSAID with an optimal efficacy/toxicity ratio and thus could be a reasonable therapeutic option for patients with painful traumatic conditions requiring parenteral NSAIDs. [4]

References:
[1]Balfour JA, Fitton A and Barradell LB.  Lornoxicam, a review of its pharmacology and therapeutic potential in the management of painful and inflammatory conditions. Drugs. 1996 Apr; 51(4): 639-57.
[2]Berg J, Fellier H, Christoph T, Grarup J and Stimmeder D.  The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro. Inflamm Res. 1999 Jul; 48(7): 369-79.
[3]Radhofer-Welte S and Rabasseda X.  Lornoxicam, a new potent NSAID with an improved tolerability profile. Drugs Today (Barc). 2000 Jan; 36(1): 55-76.
[4]Sharma A, Pingle A, and Baliga VP.  Lornoxicam efficacy in acute pain (LEAP) trial. J Indian Med Assoc. 2008 Dec; 106(12): 811-3.