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Fasudil hydrochloride semihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fasudil hydrochloride semihydrate图片
CAS NO:186694-02-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
HA-1077 hydrochloride semihydrate
AT877 hydrochloride semihydrate
产品介绍
Fasudil (HA-1077; AT877) hydrochloride semihydrate 是一种非特异性RhoA/ROCK抑制剂,并抑制蛋白激酶。Fasudil hydrochloride semihydrate 抑制ROCK1Ki为 0.33 μM,抑制ROCK2PKAPKCPKGIC50分别为 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil hydrochloride semihydrate 也是一种有效的 Ca2+通道拮抗剂和血管扩张剂。
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

PKA

4.58 μM (IC50)

p160ROCK

0.33 μM (Ki)

ROCK2

0.158 μM (IC50)

PKC

12.3 μM (IC50)

PKG

1.65 μM (IC50)

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]

Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:50 μM; 100 μM
Incubation Time:24 hours
Result:Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

RT-PCR[4]

Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:25 μM; 50 μM; 100 μM
Incubation Time:24 hours
Result:Reduced the expression of type I collagen, a-SMA, and TIMP-1.
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].

Animal Model:Myocardial ischemia and reperfusion in rat (250-300 g)[5]
Dosage:10 mg/kg
Administration:Intravenous injection; 1 h before operation
Result:Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.
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.