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别名 法舒地尔二盐酸盐, HA-1077 dihydrochloride, HA1077 dihydrochloride, AT-877 dihydrochloride, AT877 dihydrochloride
Fasudil dihydrochloride(又名 HA-1077 和 AT877)是 RhoA/ROCK 的非特异性抑制剂。其对 ROCK1(Ki = 0.33 μM)、ROCK2(IC50 = 0.158 μM)、PKA(IC50 = 4.58 μM)、PKC(IC50 = 12.30 μM)及 PKG(IC50 = 1.650 μM)具有抑制作用,同时也是一种有效的钙通道阻断剂和血管扩张剂,在血管、心血管及细胞信号研究中具有多重药理研究价值。

Fasudil dihydrochloride(又名 HA-1077 和 AT877)是 RhoA/ROCK 的非特异性抑制剂。其对 ROCK1(Ki = 0.33 μM)、ROCK2(IC50 = 0.158 μM)、PKA(IC50 = 4.58 μM)、PKC(IC50 = 12.30 μM)及 PKG(IC50 = 1.650 μM)具有抑制作用,同时也是一种有效的钙通道阻断剂和血管扩张剂,在血管、心血管及细胞信号研究中具有多重药理研究价值。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | ¥ 245 | 现货 | |
| 50 mg | ¥ 665 | 现货 | |
| 100 mg | ¥ 1,040 | 现货 |
Fasudil dihydrochloride 相关产品
| 产品描述 | Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. Fasudil dihydrochloride exhibits inhibitory effects on protein kinases including ROCK1 (Ki = 0.33 μM), ROCK2 (IC50 = 0.158 μM), PKA (IC50 = 4.58 μM), PKC (IC50 = 12.30 μM), and PKG (IC50 = 1.650 μM), while also acting as a potent Ca2+ channel blocker and vasodilator, providing a multifunctional pharmacological tool for vascular, cardiovascular, and cellular signaling research. |
| 靶点活性 | PKA:4.58 μM, PKC:12.3 μM, PKG:1.65 μM, ROCK2:0.158 μM, ROCK1 (p160ROCK):0.33 μM (Ki) |
| 体外活性 | Fasudil dihydrochloride(100 μM)可抑制大鼠肝星状细胞(HSCs)及人肝星状细胞来源的TWNT-4 细胞的铺展、应力纤维形成和α-SMA表达,同时还能显著抑制上述两种细胞的增殖 [4]。 |
| 体内活性 | Fasudil dihydrochloride(10 mg/kg,i.v.,术前1小时给药)对缺血损伤状态下的心血管系统具有保护作用,可降低JNK的活化水平,并减轻AIF的线粒体-细胞核转位 [5]。 |
| 别名 | 法舒地尔二盐酸盐, HA-1077 dihydrochloride, HA1077 dihydrochloride, AT-877 dihydrochloride, AT877 dihydrochloride |
| 分子量 | 364.29 |
| 分子式 | C14H19Cl2N3O2S |
| CAS No. | 203911-27-7 |
| Smiles | O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.Cl.Cl |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| 溶解度信息 | H2O: ≥ 80 mg/mL, Sonication is recommeded. DMSO: 16 mg/mL (43.92 mM), Sonication is recommeded. | |||||||||||||||||||||||||
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DMSO
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