计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
溶于丙酮,略溶于乙醇、氯仿、乙醚,几乎不溶于水,无味,几乎无臭。乙醇溶解度,50 mg/mL。环加氧酶(COX) 抑制剂,选择性地抑制COX-1;阻断前列腺索的生物合成。 医药上抗炎,解热作用明显,主要用于对水杨酸类药物不易耐受或疗效不显著的风湿性并节炎、强直性光脊椎炎、骨关节炎等。
Information
Indomethacin (NSC-77541, Indometacin) is a nonselectiveCOX1andCOX2inhibitor withIC50of 0.1 μg/mL and 5 μg/mL, respectively, used to reduce fever, pain, stiffness, and swelling.
In vitro
Indomethacin inhibits transcription of a beta-catenin/TCF-responsive reporter gene in a dose dependent manner. Indomethacin also downregulates the beta-catenin/TCF transcriptional target cyclin D1. Indomethacin attenuates the transcription of beta-catenin/TCF-responsive genes, by modulating TCF activity without disrupting beta-catenin/TCF complex formation.
In vivo
Indomethacin increases BrdU+ cells of all lineages and reduces microglial/monocyte activation in rats after focal cerebral ischemia. Indomethacin (7.5 mg/kg, one injection) produces acute injury and inflammation in the distal jejunum and proximal ileum that are maximal at three days and completely resolves within one week. Indomethacin (two daily subcutaneous injections) produces a more extensive and chronic inflammation that lasts in an active form in more than 75% of the rats for at least two weeks. Indomethacin (4ppm) reduces tumor yield by 78% in SKH:HR-1-hrBr hairless mice. Indomethacin (20 mg/kg, orally) increases the total area of gastric erosions and concentration of lipid peroxides in the gastric mucosa of rats. Indomethacin increases the alpha-tocopherol:total cholesterol ratio in serum. Indomethacin inhibits the increases in gastric mucosal erosions and lipid peroxides in the gastric mucosa, and the reduction of serum alpha-tocopherol.
Cell Data
cell lines:K07074 cells
Concentrations:
Incubation Time:
Powder Purity:≥99%
| ALogP | 4.3 |
|---|
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