丹参酮I  ≥98%(HPLC),分析标准品

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包装规格:20mg in glass bottle
产品简介:一种IIA型人重组sPLA2和兔重组cPLA2抑制剂,IC50分别为 11μM和82μM。
溶解性:DMSO : 2 mg/mL (7.24 mM; Need ultrasonic)
储备液保存:-80°C, 2 years -20°C, 1 year
靶点:IC50: 11 μM (sPLA2), 82 μM (cPLA2)
体外研究:Tanshinone I inhibits PGE2 formation from LPS-induced RAW macrophages (IC50=38 μM). When Tanshinone I is added simultaneously with LPS, this compound clearly inhibits PGE2 production (IC50=38 μM) at 10-100 μM. Tanshinone I also reduces PGE2 production (IC50=46 μM) when added after COX-2 is fully induced. The fact that Tanshinone I inhibits PGE2 production by pre-induced COX-2 strongly suggests that this compound may directly inhibit COX-2 activity and/or affect PLA2 activity. When Tanshinone I is incubated with two different forms of phospholipase A2 (PLA2), it clearly inhibits sPLA2 (IC50=11 μM) in a concentration-dependent manner. Although being less potent, Tanshinone I also inhibits cPLA2 (IC50=82 μM).
体内研究:Tanshinone I shows antiinflammatory activity in rat carrageenan-induced paw oedema and adjuvant-induced arthritis. In order to establish the anti-inflammatory activity of Tanshinone I, the classical animal models of acute and chronic inflammation [rat carrageenan (CGN)-induced paw oedema and rat adjuvant-induced arthritis (AIA)] are employed. When Tanshinone I is orally administered, it shows significant anti-inflammatory activity against CGN-induced paw oedema (47% inhibition at 160 mg/kg), while the IC50 of indomethacin is 7.1 mg/kg. In AIA, Tanshinone I gives 27% inhibition of secondary inflammation at 18 day with an oral dose of 50 mg/kg/day, whereas prednisolone (5 mg/kg/day) shows potent inhibition (65%).
保存条件:2-8℃
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