fasudil

Fasudil (HA-1077) 是一种非特异性 RhoA ROCK 抑制剂，也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用，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 dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].

Fasudil hydrochloride semihydrate 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64582。

Fasudil hydrochloride hydrate is an HCl salt of Fasudil -- a Rho-kinase (ROCK) inhibitor that has been shown to be effective in hindering the development of mature Cerebral Cavernous Malformation (CCM) lesions as well as reducing portal venous pressure in cirrhotic rats.

Fasudil mesylate (HA-1077; AT877) 是一种口服有效的非特异性RhoA ROCK抑制剂，同时能够抑制多种蛋白激酶。该化合物对ROCK1的Ki值为0.33 μM，对ROCK2、PKA、PKC和PKG的IC50值分别为0.158 μM、4.58 μM、12.30 μM和1.650 μM。此外，Fasudil mesylate 还作为Ca2+通道拮抗剂和血管扩张剂，表现出良好的药效。

Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA ROCK 抑制剂，也抑制蛋白激酶，对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。

Hydroxyfasudil (Hydroxy-Fasudil) 是一种ROCK 抑制剂，对ROCK1和ROCK2的IC50分别为 0.73 和 0.72 μM。

Olcorolimus inhibits single allergen-induced allergic inflammation such as eosinophilic and lymphocytic infiltration and mRNA expression for interleukin (IL)-4 and IL-5

Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) 是一种ROCK 抑制剂，对ROCK1和ROCK2的IC50值分别为 0.73 和 0.72 μM。

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

ROCK2-IN-5是一种复合型化合物，融合了Rho激酶抑制剂fasudil以及NRF2诱导剂咖啡酸和阿魏酸的结构元素。该化合物展示了优秀的多靶点作用特性和较高的耐受性。ROCK2-IN-5在针对SOD1基因变异型ALS研究中具备应用潜力。