Valdecoxib

製品コードS4049 バッチS404901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H14N2O3S
分子量 314.36 CAS No. 181695-72-7
Solubility (25°C)* 体外 DMSO 63 mg/mL (200.4 mM)
Ethanol 18 mg/mL (57.25 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension
0.5% methylcellulose 0.2% Tween 80

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 10.000mg/ml (31.81mM) Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose+0.2% Tween 80 clear solution, and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Valdecoxibは、IC50が5 nMである、強力で選択的なCOX-2阻害剤です。
in vitro Valdecoxib inhibits LPS-induced PGE2 production in plasma with IC50 of 0.89 μM for assessment of the extent of COX-2 inhibition.  This compound inhibits TxB2 production in plasma with IC50 of 25.4 μM for assessment of the extent of COX-1 inhibition. It binds to COX-2 with Ka of 1.1×105 M/s. The overall saturation binding affinity for COX-2 of this chemical is 2.6 nM. It shows similar activity in the human whole-blood COX assay (COX-2 IC50 = 0.24 μM; COX-1 IC50 = 21.9 μM). The affinity of [3H]Valdecoxib for COX-2 with KD of 3.2 nM. The binding of this compound to COX-2 seems to be both rapid and slowly reversible with association rates of 4.5 × 106/M/min and dissociation rates of 7.0 × 10-3/min (t1/2 of 98 min). The percent of dissolved this chemical at 15 min (DP15) is 10.5% for Valdecoxib and 50%, 91% and 93% for its hydrophilic derivatives (VALD-βCd, VALD-HPβCd and VALD-SBE7βCd complexes), respectively.
in vivo Valdecoxib administrated orally inhibits rat carrageenan foot pad edema with ED50 of 10.2 mg/kg. This compound administrated orally shows chronic antiinflammatory activity with ED50 of 0.032 mg/kg/day in rat adjuvant arthritis model. It shows blockade of prostaglandin production at the inflammatory site with ED50 of 0.02 mg/kg in the rat carrageenan air pouch model. This chemical demonstrates marked potency in acute and chronic models of inflammation (air pouch ED50 = 0.06 mg/kg; paw edema ED50 = 5.9 mg/kg; adjuvant arthritis ED50 = 0.03 mg/kg) in rats. It alone shows slow in vivo absorption giving maximum % inhibition of edema (16%) after a period of 3 hour. In contrast, VALD-βCd and VALD-SBE7βCd complexes shows high absorption rate in vivo achieving more than 50% inhibition of edema in the 1 hour and maximum percentage of inhibition of edema (66%) after a period of 3 hours. This compound (5 mg/kg, po) results in AUC in plasma of 3.58 μg*h/mL and 2.08 μg*h/mL in males and female mice, respectively. It (5 mg/kg, po) results in AUC red blood cells of 12.1 μg*h/mL and 6.42 μg*h/mL in males and female mice, respectively.
特徴 Valdecoxib is more potent in inhibiting COX-2 than COX-1.

プロトコル(参考用のみ)

キナーゼアッセイ COX enzyme assay in vitro
Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. This compound is preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 min before addition of arachidonic acid. PGE2 formed is detected by ELISA, after a 10 min incubation.
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 10.2 mg/kg
投与方法 Orally

参考

  • https://pubmed.ncbi.nlm.nih.gov/10715145/
  • https://pubmed.ncbi.nlm.nih.gov/15494548/
  • https://pubmed.ncbi.nlm.nih.gov/12644588/
  • https://pubmed.ncbi.nlm.nih.gov/15848054/
  • https://pubmed.ncbi.nlm.nih.gov/12642477/

カスタマーフィードバック

, , Biochem Biophys Res Commun, 2015, 460(2):198-204.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] PubMed: 35051357
On the origin of metastases: Induction of pro-metastatic states after impending cell death via ER stress, reprogramming, and a cytokine storm [ Cell Rep, 2022, 38(10):110490] PubMed: 35263600
Activating PTEN by COX-2 inhibitors antagonizes radiation-induced AKT activation contributing to radiosensitization. [Meng Z, et al. Biochem Bioph Res Co, 2015, 460(2):198-204] PubMed: 25770423

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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