伐地考昔作用机制 - Medchemexpress - MCE中国

1、Product Data SheetValdecoxibCat. No.: HY-15762CAS No.: 181695-72-7分式: CHNOS分量: 314.36作靶点: COX作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 34 mg/mL (108.16 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcen

2、tration制备储备液1 mM 3.1811 mL 15.9053 mL 31.8107 mL5 mM 0.6362 mL 3.1811 mL 6.3621 mL10 mM 0.3181 mL 1.5905 mL 3.1811 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的

3、储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.95 mM); Clear solution此案可获得 2.5 mg/mL (7.95 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 D

4、MSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.95 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (7.95 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD

5、理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.95 mM); Clear solution此案可获得 2.5 mg/mL (7.95 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Valdecoxib种效的，可服的，选择性的 COX-2 抑制剂，对 COX-2 和 COX-1 的 IC50 值分别为 5 nM 和

6、140 M，可于关节炎和疼痛的研究。IC & Target COX-2 COX-15 nM (IC50) 140 M (IC50)体外研究 Valdecoxib (Compound 2) is a highly potent, selective and orally active inhibitor of COX-2, with IC50s of 5 nM and 140M for COX-2 and COX-1, respeceively1. Valdecoxib (10, 100 M) inhibits LPS-induced proliferation of endothelialce

7、lls and bFGF secretion in a dose-dependent manner. Valdecoxib stimulates VEGF formation via HMEC-1 underinflammatory conditions2.体内研究 Valdecoxib (Compound 2) shows potent oral activity in an acute antiinflammatory assay (rat carrageenan foot padedema; ED50 = 10.2 1.4 mg/kg). Valdecoxib also has chro

8、nic antiinflammatory activity in the rat adjuvant arthritis model, with an ED50 of 0.032 0.002 mg/kg/day1. Valdecoxib (10 mg/kg, i.p.) significantly attenuates the behavioraland biochemical (oxidative damage) alterations in chronic-stressed mice3.PROTOCOLCell Assay 2 HMEC-1 cells proliferation is me

9、asured using the MTT conversion method. Cells are seeded (50.000 cells/well) into96-well plates. The cells are incubated for 24 h with LPS 100 g/mL, CoCl2 200 M, Valdecoxib 10 or 100 M, LPSand Valdecoxib or CoCl2 and Valdecoxib or without tested chemicals (control group). All the substances are adde

10、d atthe same time. After incubation, 50 L MTT (1 mg/mL) is added and the plates are incubated at 37C for 4 h. At theend of the experiment, cells are exposed to 100 L DMSO, which enables the release of the blue reaction product-formazan. The absorbance at 570 nm is read on a microplate reader and res

11、ults are expressed as a percentage of theabsorbance measured in control cells2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice3Administration 3 The drugs including naproxen (14 mg/kg, i.p.), rofecoxib (5 mg/kg, i.p.), meloxicam (5 mg/kg, i.p

12、.), nimesulide (5mg/kg, i.p.) and Valdecoxib (10 mg/kg, i.p.) are used in the assay. The animals are randomized into 7 groups (n=10in each group), including the naive group, in which the mice only receive vehicle for 15 d without forced swimmingsession; the control (chronically stressed) group, in w

13、hich mice receive vehicle 30 min before the forced swimmingsession (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 (CM

14、C) and administered intraperitoneally, 30 min before the forced swimming session for15 consecutive days3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 J Pharm Biomed Anal. 2018 May 22;158:1-7.See more customer valid

15、ations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. 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 Mar9;43(5):775-7.2. Wiktorowska-Owczarek A. The effect of valdecoxib on the production of growth factors evoked by hypoxia and bacterial lipopolysaccharide in HMEC-1cells. Adv Clin Exp Med. 2013 Nov-Dec;22(6):795-800.3. Kumar A, et al. Protective effects of selective and non-selective cyclooxygenase inhibitors in an animal model of chronic stress. Neurosci Bull. 20