型号:
产品价格:电议      采购度:1596      原产地:美洲
发布时间:2021/7/24 0:06:08 所属地区:上海 上海市
简要描述:
Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride) 是一种非特异性 RhoA/ROCK 抑制剂,对蛋白激酶也有抑制作用,ROCK1 的 Ki 值为 μM,ROCK2 和 PKA,PKC,PKG 的 IC50 值分别 μM 和 μM, μM, μM。Fasudil Hydrochloride 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。
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CAS No. : 105628-07-7
MCE 站:Fasudil Hydrochloride
产品活性:Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride) 是一种非特异性 RhoA/ROCK 抑制剂,对蛋白激酶也有抑制作用,ROCK1 的 Ki 值为 0.33 μM,ROCK2 和 PKA,PKC,PKG 的 IC50 值分别 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil Hydrochloride 也是一种有效的 Ca2+ 通道拮抗剂和血管扩张剂。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad | Neuronal Signaling | Membrane Transporter/Ion Channel | Autophagy | Protein Tyrosine Kinase/RTK | Epigenetics | Anti-infection
作用靶点:ROCK | Calcium Channel | Autophagy | PKA | PKC | HIV
In Vitro: Fasudil Hydrochloride (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs and human HSC-derived TWNT-4 cells.Fasudil Hydrochloride (50-100 μM; 24 hours) inhibits the LPA-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells.Fasudil Hydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells.
In Vivo: Fasudil (30 μg) increases CBF by 50% via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (100 mg/kg/day, p.o.) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration.
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更新时间:2024/1/2 10:14:29
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