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编 号:F741812
分子式:C13H11NO4
分子量:245.23
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生物活性:
COX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects.

体内研究:
COX-2-IN-34 (compound 8a) ( 口服, 50 mg/kg, 三天) 在正常雄性大鼠模型中无胃溃疡毒性。COX-2-IN-34 (皮下注射, 50 mg/kg) 在卡拉胶诱导的大鼠足跖水肿实验模型中表现出明显的抗炎作用。Animal Model:The Carrageenan-induced rat paw edema assay model
Dosage:50 mg/kg
Administration:Subcutaneous injection (s.c.)
Result:Expressed the reduction of edema claw volume after 0h, 1 h, 2 h, 3h, 4 h, and 6 h of carrageenan injection compared to the control group. Exhibited superior inhibition of 42.90% and 45.95% at the 3rd and 4th hour, respectively, which was comparatively much closer in potency to that of the Celecoxib (HY-14398) group (45.18% inhibition of edema at 3h).

体外研究:
COX-2-IN-34 (compound 8a) (100 μM, 24 h) 对 RAW264.7 细胞没有明显的细胞毒性。COX-2-IN-34 选择性抑制 COX-1 和 COX-2 活性,其 IC50 分别为 34.86 和 0.42 μM。10 μM 的 COX-2-IN-34 对 COX-2 的抑制效果达到 82%。
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