Lornoxicam
(Synonyms: 氯诺昔康; Chlortenoxicam; Ro 13-9297) 目录号 : GC13572
A COX inhibitor and NSAID
Cas No.:70374-39-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 70374-39-9 | SDF | |
| 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 SMILES | CN1C(=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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6895 mL | 13.4474 mL | 26.8947 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet