CAS NO: | 103745-39-7 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Fasudil (HA-1077; AT877) is a nonspecificRhoA/ROCKinhibitor and also has inhibitory effect on protein kinases, with anKiof 0.33 μM forROCK1,IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM forROCK2andPKA,PKC,PKG, respectively. Fasudil is also a potent Ca2+channel antagonist and vasodilator[1][2][3]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4].Fasudil (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4].Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4]. Western Blot Analysis[4]
RT-PCR[4]
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体内研究 (In Vivo) | Fasudil (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[5].Fasudil (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio[6].Fasudil (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice[6].
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Clinical Trial | |||||||||||||||||
分子量 | 291.37 | ||||||||||||||||
Formula | C14H17N3O2S | ||||||||||||||||
CAS 号 | 103745-39-7 | ||||||||||||||||
中文名称 | 法舒地尔 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |