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Ampiroxicam

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Chemical Structure| 99464-64-9 同义名 : 氨吡昔康 ;CP 65703;CP 65,703;Ampiroxicamum;Flucam
CAS号 : 99464-64-9
货号 : A149917
分子式 : C20H21N3O7S
纯度 : 98%
分子量 : 447.462
MDL号 : MFCD00866079
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(111.74 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
靶点

  • COX
描述 Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug. Ampiroxicam is a nonacidic ether carbonate prodrug of piroxicam. In an acute model of paw inflammation in rats, ampiroxicam is less potent than piroxicam itself: the ED50's of ampiroxicam are 9- and 3.5-fold higher than those of piroxicam following a single or multiple (5) daily oral doses, respectively[3]. Ampiroxicam inhibits the stretching response in mice induced by phenylbenzoquinone (PBQ) with maximum protective effect (MPE) of 2 mg/kg. Ampiroxicam inhibits swelling in a dose-responsive manner in the rat foot edema (RFE) assay with ED50 of 28 mg/kg at single oral dose and 7.8 mg/kg at 5 daily oral dose. Ampiroxicam blocks primary and secondary lesion development in rat adjuvant arthritis with ED50 of 2.2 mg/kg and 0.5 mg/kg, respectively. Ampiroxicam (3.2 mg/kg) leads to a plasma concentration of 12 μg/mL at a Tmax of 2 hours in rats[4]. Ultraviolet-A (UVA) -irradiated 1% Ampiroxicam sensitized in guinea pigs shows positive reaction in the patch testing to UVA-irradiated 1% Ampiroxicam and 1% thiosalicylate (TOS). Concentration of Ampiroxicam is easily reduced by the increase in UVA irradiation doses, as compared with that of piroxicam[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.35mL

4.47mL

2.23mL
参考文献

[1]Abdelrahim M, Baker CH, et al. Regulation of vascular endothelial growth factor receptor-1 expression by specificity proteins 1, 3, and 4 in pancreatic cancer cells. Cancer Res. 2007 Apr 1;67(7):3286-94.

[2]Abdelrahim M, Baker CH, et al. Tolfenamic acid and pancreatic cancer growth, angiogenesis, and Sp protein degradation. J Natl Cancer Inst. 2006 Jun 21;98(12):855-68.

[3]Carty TJ, Marfat A, Moore PF, Falkner FC, Twomey TM, Weissman A. Ampiroxicam, an anti-inflammatory agent which is a prodrug of piroxicam. Agents Actions. 1993 Jul;39(3-4):157-65

[4]Aoki T, Yamaguchi H, Naito H, Shiiki K, Izawa K, Ota Y, Sakamoto H, Kaneko A. Premedication with cyclooxygenase-2 inhibitor meloxicam reduced postoperative pain in patients after oral surgery. Int J Oral Maxillofac Surg. 2006 Jul;35(7):613-7

[5]Sasaki T, Shimizu H, Tokuyama S, Hariya T, Soh I, Sueki H, Iijima M, Yamamoto T, Kuroiwa Y. Antigenic characterization in ampiroxicam-induced photosensitivity using an in vivo model of contact hypersensitivity. J Dermatol Sci. 1999 Nov;21(3):170-5