Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC₅₀s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.

Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC₅₀s of 5 nM and 140 μM for COX-2 and COX-1, respeceively^[1]. Valdecoxib (10, 100 µM) inhibits LPS-induced proliferation of endothelial cells and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 under inflammatory conditions^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot pad edema; ED₅₀ = 10.2 ± 1.4 mg/kg). Valdecoxib also has chronic antiinflammatory activity in the rat adjuvant arthritis model, with an ED₅₀ of 0.032 ± 0.002 mg/kg/day^[1]. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioral and biochemical (oxidative damage) alterations in chronic-stressed mice^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

314.36

C₁₆H₁₄N₂O₃S

181695-72-7

固体

White to off-white

伐地昔布

• Others

• 内源性代谢物

Room temperature in continental US; may vary elsewhere.

DMSO 中的溶解度 : ≥ 34 mg/mL (108.16 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* “≥” means soluble, but saturation unknown.

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• 方案 一

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

  Solubility: ≥ 2.5 mg/mL (7.95 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

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

  Solubility: ≥ 2.5 mg/mL (7.95 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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。

  20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

• 方案 三

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.5 mg/mL (7.95 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Talley JJ, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7.  [Content Brief]

  [2]. Wiktorowska-Owczarek A. The effect of valdecoxib on the production of growth factors evoked by hypoxia and bacterial lipopolysaccharide in HMEC-1 cells. Adv Clin Exp Med. 2013 Nov-Dec;22(6):795-800.  [Content Brief]

  [3]. Kumar A, et al. Protective effects of selective and non-selective cyclooxygenase inhibitors in an animal model of chronic stress. Neurosci Bull. 2010 Feb;26(1):17-27.  [Content Brief]

HMEC-1 cells proliferation is measured using the MTT conversion method. Cells are seeded (50.000 cells/well) into 96-well plates. The cells are incubated for 24 h with LPS 100 µg/mL, CoCl₂ 200 µM, Valdecoxib 10 or 100 µM, LPS and Valdecoxib or CoCl₂ and Valdecoxib or without tested chemicals (control group). All the substances are added at the same time. After incubation, 50 µL MTT (1 mg/mL) is added and the plates are incubated at 37°C for 4 h. At the end of the experiment, cells are exposed to 100 µL DMSO, which enables the release of the blue reaction product-formazan. The absorbance at 570 nm is read on a microplate reader and results are expressed as a percentage of the absorbance measured in control cells^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[3]
The drugs including naproxen (14 mg/kg, i.p.), rofecoxib (5 mg/kg, i.p.), meloxicam (5 mg/kg, i.p.), nimesulide (5 mg/kg, i.p.) and Valdecoxib (10 mg/kg, i.p.) are used in the assay. The animals are randomized into 7 groups (n=10 in each group), including the naive group, in which the mice only receive vehicle for 15 d without forced swimming session; the control (chronically stressed) group, in which mice receive vehicle 30 min before the forced swimming session (6 min) for 15 d; the naproxen (14 mg/kg) group; the Valdecoxib (10 mg/kg) group; the rofecoxib (5 mg/kg) group; the meloxicam (5 mg/kg) group; and the nimesulide (5 mg/kg) group. Drugs are suspended in 0.25% carboxymethylcellulose (CMC) and administered intraperitoneally, 30 min before the forced swimming session for 15 consecutive days^[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Talley JJ, et al. 4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2. J Med Chem. 2000 Mar 9;43(5):775-7.  [Content Brief]

  [2]. Wiktorowska-Owczarek A. The effect of valdecoxib on the production of growth factors evoked by hypoxia and bacterial lipopolysaccharide in HMEC-1 cells. Adv Clin Exp Med. 2013 Nov-Dec;22(6):795-800.  [Content Brief]

  [3]. Kumar A, et al. Protective effects of selective and non-selective cyclooxygenase inhibitors in an animal model of chronic stress. Neurosci Bull. 2010 Feb;26(1):17-27.  [Content Brief]