| 生化机理 |
SLx-2119 selectively inhibits activity of human ROCK2 (IC50 = 105 nM), while effects on human ROCK1 in this cell-free system were minimal (IC50 = 24 μM). SLx-2119 at 40 μM induced significant down-regulations of Tsp-1 and CTGF mRNA levels. SLx-2119 induced a significant down-regulation of Tsp-1 transcripts in HMVEC and PASMC only and induced a down-regulation of CTGF transcripts, although non-significant, in all 3 cell types(HMVEC, PASMC, and NHDF). SLx-2119 induced a down-regulation of the genes COL1A1, COL1A2, COL3A1, and COL5A2 in PASMC, an up-regulation of the gene MMP1 in PASMC, a down-regulation of the gene COL3A1 in NHDF, and an up-regulation of the genes COL7A1, COL4A2, MMP1, MMP3, MMP14, and MMP17 in NHDF. |
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