ロルノキシカム
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Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.58%
- CAS 番号: 70374-39-9
- 分子式: C13H10ClN3O4S2
- 分子量:371.82
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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COX-1 5 nM (IC50, in cells) |
COX-2 45 nM (IC50, in cells) |
Lornoxicam (0.03-3 μM; 24 h) dose-dependently inhibites the formation of TXB2 in HEL cells, the formation of PGF1 in Mono Mac 6 cells stimulated by LPS (HY-D1056) and the accumulation of NO in the supernatant of RAW 264.7 cells stimulated by LPS (HY-D1056)[6]. Lornoxicam (10-300 μM; 10 min) dose-dependently inhibites the formation of IL-6 in human monocytic THP-1 cells (IC50=54 μM) and weakly stimulates the production of TNF-a, IL-1b and IL-8 at a dose of 300 μM[6]. Lornoxicam (3.1-400 μg/mL; 0-48 h) concentration-dependently induces a decrease in the viability of cervical cancer, colorectal cancer, and breast cancer cell lines HeLa, MCF-7, and HT-29 and inhibites the proliferation of HT-29 cell line[7]. Lornoxicam (400 μg/mL; 24 h) induces apoptosis in HT-29 and MCF-7 tumor cells[7]. Lornoxicam (400 μg/mL; 0-72 h) inhibites the migration of HT-29 and MCF-7 tumor cells[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, MCF-7 and HT-29 tumor cell lines
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Concentration:3.1, 6.3, 12.5, 25, 50, 100, 200 and 400 μg/mL
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Incubation Time:24 and 48 h
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Result:Induced a statistically significant reduction of the viability of HeLa tumor cells only at concentrations of 200 μg/mL and 400 μg/mL after 24 h and at all tested concentrations after 48 h of exposure.
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Cell Line:HT-29 tumor cell lines
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Concentration:3.1, 6.3, 12.5, 25, 50, 100, 200 and 400 μg/mL
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Incubation Time:24 and 48 h
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Result:Antiproliferative effects of lornoxicam on HT-29 cells at concentrations of 100, 200, and 400 μg/mL.
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Cell Line:HT-29 and MCF-7 tumor cell lines
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Concentration:400 μg/mL
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Incubation Time:24 h
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Result:Induced morphological characteristics of early and late apoptosis in HT-29 cells. Led to condensation and margination of chromatin in the nuclei of MCF-7 cells.
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Cell Line:HT-29 and MCF-7 tumor cell lines
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Concentration:400 μg/mL
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Incubation Time:24, 48 and 72 h
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Result:The migration percentages of HT-29 tumor cell were 12.34%, 18.28%, and 18.61% at 24, 48 and 72 h. The migration percentages of MCF-7 tumor cell were 3.85%, 7.77%, and 9.06% at 24, 48 and 72 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with thermal hind paw hyperalgesia model induced by tail injection of 10% formaldehyde[3].
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Dosage:1.3 mg/kg
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Administration:Intraperitoneal injection (i.p.); Single dose injection 30 minutes before 10% formaldehyde
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Result:Produced anti-inflammatory effects, did not alter thermal nociceptive thresholds, and completely blocked hindlimb hyperalgesia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 70374-39-9
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性状 Solid
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分子量 371.82
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分子式 C13H10ClN3O4S2
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Color Light yellow to yellow
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SMILES
O=C(C1=C(O)C2=C(C=C(Cl)S2)S(N1C)(=O)=O)NC3=NC=CC=C3
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別名
Lornoxicam; Chlortenoxicam; Ro 13-9297
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 3.8 mg/mL (10.22 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (281 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Spyra S, et al. COX-2-selective inhibitors celecoxib and deracoxib modulate transient receptor potential vanilloid 3 channels. Br J Pharmacol. 2017 Aug;174(16):2696-2705. [Content Brief]
[2]. Rose, P. and C. Steinhauser, Comparison of Lornoxicam and Rofecoxib in Patients with Activated Osteoarthritis (COLOR Study). Clin Drug Investig, 2004. 24(4): p. 227-36. [Content Brief]
[3]. Bianchi, M. and A.E. Panerai, Effects of lornoxicam, piroxicam, and meloxicam in a model of thermal hindpaw hyperalgesia induced by formalin injection in rat tail. Pharmacol Res, 2002. 45(2): p. 101-5. [Content Brief]
[4]. Balfour J A, et al. Lornoxicam: a review of its pharmacology and therapeutic potential in the management of painful and inflammatory conditions[J]. Drugs, 1996, 51: 639-657. [Content Brief]
[5]. Pohlmeyer-Esch G, et al. Evaluation of chronic oral toxicity and carcinogenic potential of lornoxicam in rats[J]. Food and chemical toxicology, 1997, 35(9): 909-922. [Content Brief]
[6]. Berg J, et al. The analgesic NSAID lornoxicam inhibits cyclooxygenase (COX)-1/-2, inducible nitric oxide synthase (iNOS), and the formation of interleukin (IL)-6 in vitro[J]. Inflammation Research, 1999, 48: 369-379. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6895 mL | 13.4474 mL | 26.8947 mL | 67.2368 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL | 13.4474 mL | |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 mL | 6.7237 mL |
Lornoxicam 関連分類
HY-B0367 関連分類
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