CAS NO: | 186694-02-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Fasudil (HA-1077; AT877) hydrochloride semihydrate 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 hydrochloride semihydrate is also a potent Ca2+channel antagonist and vasodilator[1][2][3]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Fasudil hydrochloride semihydrate (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 hydrochloride semihydrate (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 hydrochloride semihydrate (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 hydrochloride semihydrate (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 hydrochloride semihydrate (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 hydrochloride semihydrate (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 | 673.68 | ||||||||||||||||
Formula | C14H19ClN3O2.5S | ||||||||||||||||
CAS 号 | 186694-02-0 | ||||||||||||||||
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. |