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Ampiroxicam

CAS号

99464-64-9

分子式

C20H21N3O7S

主要靶点

COX

仅限科研使用

Cat No : CM03531

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Synonyms

inhibit|Flucam|Cyclooxygenase|COX|CP 65703|CP65703|CP-65703|Ampiroxicam|安吡昔康|Inhibitor

验证数据展示

  • CAS No.: 99464-64-9

    Ampiroxicam
    CAS#: 99464-64-9

产品信息

CAS号 99464-64-9
分子式 C20H21N3O7S
主要靶点 COX
主要通路 免疫与炎症|神经科学
分子量 447.46
纯度 99.2%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 inhibit|Flucam|Cyclooxygenase|COX|CP 65703|CP65703|CP-65703|Ampiroxicam|安吡昔康|Inhibitor

体内活性

Ampiroxicam通过抑制小鼠对苯酚醌(PBQ)引起的拉伸反应，展现出最大保护效果(MPE)为2 mg/kg。Ampiroxicam在大鼠足肿胀(RFE)实验中以剂量依赖的方式抑制肿胀，单次口服剂量的ED50为28 mg/kg，连续5天口服剂量的ED50为7.8 mg/kg。在大鼠关节炎模型中，Ampiroxicam阻断了一级和二级病变的发展，其ED50分别为2.2 mg/kg和0.5 mg/kg。Ampiroxicam (3.2 mg/kg)在大鼠体内转化为piroxicam后，可在2小时达到最大血浆浓度(Tmax)为12 μg/mL。[3]在豚鼠身上，1% Ampiroxicam经紫外线A (UVA)辐照后，在斑贴试验中对经UVA辐照的1% Ampiroxicam和1%硫代水杨酸(TOS)产生了阳性反应。与piroxicam相比，Ampiroxicam的浓度更容易通过增加UVA辐照剂量而减少。[4]

体外活性

Ampiroxicam (<150 μM) 剂量依赖性地减少了Panc-1细胞的增殖。[1] Ampiroxicam (50 μM) 导致Panc-1细胞和L3.6pl细胞中Sp1、Sp3、Sp4和VEGFR1蛋白表达下降，通过Western blot分析确定。同时，Ampiroxicam (50 μM) 导致在Panc-1细胞和L3.6pl细胞中MAPK1/2的磷酸化增加。[2]

溶解度

DMSO:83 mg/mL (185.5 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

Panc-1 cells are plated in DME/F12 medium with 5% fetal bovine serum and treated on the next day with vehicle (0.1% DMSO) or various concentrations of Ampiroxicam. Cells are counted at the indicated times with a Coulter Z1 cell counter. Each experiment is done in triplicate, and results are expressed as means, with error bars representing 95% confidence intervals (CIs).(Only for Reference)

参考文献

1.Abdelrahim M, et al. J Natl Cancer Inst, 2006, 98(12), 855-868.
2.Abdelrahim M, et al. Cancer Res, 2007, 67(7), 3286-3294.
3.Carty TJ, et al. Agents Actions, 1993, 39(3-4), 157-165.
4.Sasaki T, et al. J Dermatol Sci, 1999, 21(3), 170-175.

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