Lumiracoxib(Synonyms: 罗美昔布; COX-189)

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Lumiracoxib (Synonyms: 罗美昔布; COX-189) 纯度: 99.65%

Lumiracoxib 是一种强效、选择性、口服活性 COX-2 抑制剂，Ki 值为 0.06 μM。Lumiracoxib 是一种非选择性非甾体抗炎试剂 (NSAID)，具有抗炎、解热活性。Lumiracoxib 可用于骨关节炎和骨癌研究。

Lumiracoxib(Synonyms: 罗美昔布; COX-189)

Lumiracoxib Chemical Structure

CAS No. : 220991-20-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥800 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Lumiracoxib is a potent,selective and orally active COX-2 inhibitor with a Ki value of 0.06 μM[1]. Lumiracoxib acts as a nonselective NSAID with anti-inflammatory, analgesic and antipyretic activities. Lumiracoxib can be used for osteoarthritis and bone cancer research[1][2].

IC50 & Target

COX-2

0.06 μM (Ki)

COX-1

3 μM (Ki)

体外研究
(In Vitro)

Lumiracoxib inhibits purified COX-1 and COX-2 with Ki values of 3 μM and 0.06 μM, respectively. In cellular assays, Lumiracoxib has an IC50 of 0.14 μM in COX-2-expressing dermal fibroblasts, but causesno inhibition of COX-1 at concentrations up to 30 μM in HEK293 cells transfected with human COX-1[1].
In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Lumiracoxib (oral administration; 10 and 30 mg/kg; single dose) significantly reverses the established hyperalgesia with a maximal 58% reversal observed 3 h following administration in rat model[1].
Lumiracoxib (oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection) significantly attenuates the weight-bearing difference observed on days 14, 17 and 20. The repeated administration significantly reverses static allodynia measured 90 min following the final administration.It significantly reduces the radiologically observed structural changes 20 days after inoculation of MRMT-1 cells in rat[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat model of bone cancer pain with injection of MRMT-1 tumour cells into one tibia[1] 
Dosage: 10 and 30 mg/kg
Administration: Oral administration; 10 and 30 mg/kg; twice daily; from day 10 to day 20 following MRMT-1 cell injection
Result: Had an effect on mechanical hyperalgesia in a model of bone cancer pain.

Clinical Trial

分子量

293.72

Formula

C15H13ClFNO2
CAS 号

220991-20-8
中文名称

罗美昔布
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (425.58 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4046 mL 17.0230 mL 34.0460 mL
5 mM 0.6809 mL 3.4046 mL 6.8092 mL
10 mM 0.3405 mL 1.7023 mL 3.4046 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (7.08 mM); Clear solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (7.08 mM) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.08 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ronald Esser, et al. Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2. Br J Pharmacol. 2005 Feb;144(4):538-50.

    [2]. Alyson Fox, et al. Anti-hyperalgesic activity of the cox-2 inhibitor lumiracoxib in a model of bone cancer pain in the rat. Pain

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