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Valdecoxib(SC65872)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Valdecoxib(SC65872)图片
CAS NO:181695-72-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)314.36
FormulaC16H14N2O3S
CAS No.181695-72-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 63 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 18 mg/mL (57.2 mM)
Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 19 mg/mL
SynonymsSC-65872; SC 65872; Bextra; SC65872;
实验参考方法
In Vitro

In vitro activity: Valdecoxib inhibits LPS-induced PGE2 production in plasma with IC50 of 0.89 μM for assessment of the extent of COX-2 inhibition. Valdecoxib inhibits TxB2 production in plasma with IC50 of 25.4 μM for assessment of the extent of COX-1 inhibition. Valdecoxib binds to COX-2 with Ka of 1.1×105 M/s. The overall saturation binding affinity for COX-2 of Valdecoxib is 2.6 nM. Valdecoxib 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 Valdecoxib 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 Valdecoxib 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.


Cell Assasy: 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


In Vivo
Valdecoxib administrated orally inhibits rat carrageenan foot pad edema with ED50 of 10.2 mg/kg. Valdecoxib administrated orally shows chronic antiinflammatory activity with ED50 of 0.032 mg/kg/day in rat adjuvant arthritis model. Valdecoxib administrated orally shows blockade of prostaglandin production at the inflammatory site with ED50 of 0.02 mg/kg in the rat carrageenan air pouch model. Valdecoxib 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. Valdecoxib 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. Valdecoxib (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. Valdecoxib (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.
Animal modelMale Sprague-Dawley rats
Formulation & DosageFormulated in 0.5% methyl cellulose and 0.025% Tween-20; 10.2 mg/kg; Oral gavage
References

J Med Chem. 2000 Mar 9;43(5):775-7; J Pharmacol Exp Ther. 2005 Mar;312(3):1206-12.