1. Immunology/Inflammation
  2. COX
  3. Lumiracoxib

Lumiracoxib  (Synonyms: COX-189; ルミラコキシブ)

製品番号: HY-13507 純度: 99.56%
COA 取扱説明書 Technical Support

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

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Lumiracoxib

Lumiracoxib 構造式

CAS 番号 : 220991-20-8

容量 価格(税別) 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
5 mg $25 在庫あり
10 mg $40 在庫あり
25 mg $80 在庫あり
50 mg $128 在庫あり
100 mg $192 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

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製品説明

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[1]

COX-2

0.06 μM (Ki)

COX-1

3 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
Fibroblast IC50
130 nM
Compound: 1, lumiracoxib
Inhibition of human COX2 mediated PGE2 production in IL-1-beta-induced human dermal fibroblast cells
Inhibition of human COX2 mediated PGE2 production in IL-1-beta-induced human dermal fibroblast cells
[PMID: 17434872]
体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) 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.
臨床実験
分子量

293.72

分子式

C15H13ClFNO2

CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 125 mg/mL (425.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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体積 (開始)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.93%

参考文献

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4046 mL 17.0230 mL 34.0460 mL 85.1151 mL
5 mM 0.6809 mL 3.4046 mL 6.8092 mL 17.0230 mL
10 mM 0.3405 mL 1.7023 mL 3.4046 mL 8.5115 mL
15 mM 0.2270 mL 1.1349 mL 2.2697 mL 5.6743 mL
20 mM 0.1702 mL 0.8512 mL 1.7023 mL 4.2558 mL
25 mM 0.1362 mL 0.6809 mL 1.3618 mL 3.4046 mL
30 mM 0.1135 mL 0.5674 mL 1.1349 mL 2.8372 mL
40 mM 0.0851 mL 0.4256 mL 0.8512 mL 2.1279 mL
50 mM 0.0681 mL 0.3405 mL 0.6809 mL 1.7023 mL
60 mM 0.0567 mL 0.2837 mL 0.5674 mL 1.4186 mL
80 mM 0.0426 mL 0.2128 mL 0.4256 mL 1.0639 mL
100 mM 0.0340 mL 0.1702 mL 0.3405 mL 0.8512 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

製品名:
Lumiracoxib
製品番号:
HY-13507
数量:
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