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体外研究 (In Vitro) |
吲哚美辛(Indometacin)(0-150 μM;24 小时;3LL-D122 细胞)的体外抗肿瘤活性已有报道[2]。通过激活 PKR 和磷酸化 eF2α,吲哚美辛 (Indometacin) (0-1000 μM) 抑制病毒复制 (IC50=2 μM) 并停止病毒蛋白翻译,保护宿主细胞免受病毒伤害 [3]。当暴露于 8 μM 吲哚美辛 26 小时时,M1 型 RAW 264.7 细胞会发生 M2 型分化 [4]。当人类脂肪干细胞暴露于吲哚美辛 (200 μM) 五天时,会转分化为神经源性样细胞 [5]。
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体内研究 (In Vivo) |
使用吲哚美辛,可以在动物身上建立胃肠道溃疡模型。
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动物实验 |
Animal/Disease Models: Male SD (Sprague-Dawley) rats[1]
Doses: 0.01-10 mg/kg Route of Administration: Oral administration; for 3 hrs (hours) Experimental Results: Inhibited the carrageenan-induced rat paw oedema (ED50=2.0 mg/kg) and hyperalgesia (ED50= 1.5 mg/kg) in a dose-dependent manner. Animal/Disease Models: Male C57BL/6J mice[2] Doses: 10 mg/mL Route of Administration: Oral administration; daily, for 29 days Experimental Results: Delayed the onset of tumor growth and the initial growth rate of the footpad tumors. |
参考文献 |
[1]. Riendeau D, et, al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.
[2]. Eli Y, et, al. Comparative effects of indomethacin on cell proliferation and cell cycle progression in tumor cells grown in vitro and in vivo. Biochem Pharmacol. 2001 Mar 1;61(5):565-71. [3]. Amici C, et, al. Inhibition of viral protein translation by indomethacin in vesicular stomatitis virus infection: role of eIF2α kinase PKR. Cell Microbiol. 2015 Sep;17(9):1391-404. [4]. Luo X, Xiong H, Jiang Y, et al. Macrophage Reprogramming via Targeted ROS Scavenging and COX-2 Downregulation for Alleviating Inflammation. Bioconjug Chem. 2023;34(7):1316-1326. [5]. Kompisch KM, Lange C, Steinemann D, et al. Neurogenic transdifferentiation of human adipose-derived stem cells? A critical protocol reevaluation with special emphasis on cell proliferation and cell cycle alterations. Histochem Cell Biol. 2010;134(5):453-468. |
分子式 |
C19H16CLNO4
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分子量 |
357.79
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CAS号 |
53-86-1
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相关CAS号 |
Indomethacin;53-86-1;Indomethacin sodium hydrate;74252-25-8
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SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C(N1C(C([H])([H])[H])=C(C([H])([H])C(=O)O[H])C2C([H])=C(C([H])=C([H])C1=2)OC([H])([H])[H])=O
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InChi Key |
CGIGDMFJXJATDK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H16ClNO4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9H,10H2,1-2H3,(H,22,23)
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化学名 |
2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid
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别名 |
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7949 mL | 13.9747 mL | 27.9494 mL | |
5 mM | 0.5590 mL | 2.7949 mL | 5.5899 mL | |
10 mM | 0.2795 mL | 1.3975 mL | 2.7949 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。