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Amfenac Sodium Hydrate

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Chemical Structure| 61618-27-7 同义名 : 氨芬酸钠一水合物 ;Amfenac Sodium Monohydrate;Amfenac (sodium salt hydrate)
CAS号 : 61618-27-7
货号 : A120991
分子式 : C15H14NNaO4
纯度 : 98%+
分子量 : 295.266
MDL号 : MFCD00941383
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(491.08 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(169.34 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • COX-2

    COX-2, IC50:150 nM

  • COX-1

    COX-1, IC50:250 nM
描述 Amfenac Sodium Monohydrate is a COX-2 (cyclooxygenase-2) inhibitor. Amfenac affected both COX-2 transfected and non-transfected uveal melanoma cells in terms of their proliferation rates as well as their suppressive effects on macrophage cytotoxic activity[3]. Treatment of UM (uveal melanoma) cell lines with amfenac prior to radiation led to a marked reduction in proliferation rates. There appears to be a radioprotective effect of amfenac on human fibroblasts[4]. 5×10-4 M Amfenac Sodium Hydrate inhibits the release of the enzyme 35.3 and 16.3% in the presence of 10-8, and 10-7 M FMLP, respectively. Addition of 10-4 M Amfenac Sodium Hydrate causes 28.3% inhibition of aggregation of polgmorphonuclear leukocgtes (PMNs) during incubation for 16 min with 10-8 M FMLP[5]. Moreover, Amfenac treatment significantly inhibited VEGF-induced tube formation and proliferation by EC. Amfenac treatment significantly reduced retinal prostanoid production and NV (neovascularization) in OIR[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.87mL

6.77mL

3.39mL
参考文献

[1]Gamache DA, Graff G, et al. Nepafenac, a unique nonsteroidal prodrug with potential utility in the treatment of trauma-induced ocular inflammation: I. Assessment of anti-inflammatory efficacy. Inflammation. 2000 Aug;24(4):357-70.

[2]Sancilio LF, Reese DL, et al. AHR-5850: a potent anti-inflammatory compound. Agents Actions. 1977 Mar;7(1):133-44.

[3]Marshall JC, Caissie AL, Cruess SR, Cools-Lartigue J, Burnier MN Jr. The effects of a cyclooxygenase-2 (COX-2) expression and inhibition on human uveal melanoma cell proliferation and macrophage nitric oxide production. J Carcinog. 2007;6:17. Published 2007 Nov 27

[4]Fernandes BF, Marshall JC, Di Cesare S, Logan P, Maloney S, Burnier MN Jr. Amfenac increases the radiosensitivity of uveal melanoma cell lines. Eye (Lond). 2008;22(5):701-706

[5]Matsumoto T, Yuda Y, Sekizawa Y, Takano T. Effect of a non-steroidal anti-inflammatory drug (amfenac sodium) on polymorphonuclear leukocytes. Pharmacol Res Commun. 1982;14(6):523-532

[6]Yanni SE, Clark ML, Yang R, Bingaman DP, Penn JS. The effects of nepafenac and amfenac on retinal angiogenesis. Brain Res Bull. 2010;81(2-3):310-319