生物活性 | |||
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描述 | Fasudil hydrochloride semihydrate is a non-specific RhoA/ROCK inhibitor, which also inhibits protein kinases, with a Ki of 0. 33 μM for ROCK1, and IC50s of 0. 158 μM and 4. 58 μM for ROCK2 and 12. 30 μM for PKA, PKC, and PKG, respectively, Fasudil hydrochloride semihydrate is also a potent Ca2+ channel antagonist and vasodilator[1][2][3]. Fasudil hydrochloride semihydrate at a concentration of 100 μM inhibited cell spreading, stress fibre formation and α-SMA expression in rat haematopoietic stem cells (hepatic stellate cells) and human haematopoietic stem cell-derived TWNT-4 cells, as well as inhibiting cell growth. Fasudil hydrochloride semihydrate in the concentration range of 50-100 μM for 24 hours was shown to inhibit cell growth. Fasudil hydrochloride semihydrate at 50-100 μM for 24 hours inhibited LPA (lysophosphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38. Fasudil hydrochloride semihydrate at 25-100 μM for 24 hours inhibited the transcription of collagen and TIMP, and stimulated the transcription of MMP-1 in human haematopoietic stem cell-derived TWNT-4 cells[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.48mL 0.30mL 0.15mL |
7.42mL 1.48mL 0.74mL |
14.84mL 2.97mL 1.48mL |