Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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50 mg | 在庫あり | ¥ 8,000 | |||
100 mg | 在庫あり | ¥ 10,500 | |||
200 mg | 在庫あり | ¥ 16,000 | |||
500 mg | 在庫あり | ¥ 22,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,500 |
説明 | Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. |
ターゲット&IC50 | ROCK1:0.33 μM(ki), PKC:9.3 μM(ki), PKA:1.0 μM(ki), MLCK:55 μM(ki) |
In vitro | Intravenous injections of Fasudil at doses of 0.01, 0.03, 0.1, and 0.3 mg/kg decreased mean blood pressure (MBP) and increased heart rate (HR), vertebral blood flow (VBF), cerebral blood flow (CBF), renal blood flow (RBF), and femoral blood flow (FBF) in a dose-dependent manner. A total Fasudil dose of 1.0 ng/mL enhanced cardiac output. Intracoronary injections of 30 μg Fasudil in experimental dogs resulted in approximately a 50% increase in CBF. Oral administration of Fasudil (dose of 100 mg/kg/day) significantly lowered the incidence and average maximum clinical score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice immunized with PLP p139-151. Fasudil inhibited the proliferation response of mouse spleen cells to antigens, demonstrating cardiovascular protective effects by reducing the activation of JNK and mitigating the mitochondrial translocation of apoptosis-inducing factor (AIF) in ischemic injury. |
In vivo | Fasudil induces the disassembly of actomyosin fibers and inhibits cell migration, competitively suppressing Ca2+-induced depolarization and constriction of the rabbit aorta. It blocks contraction responses to KCl, serum phenylalanine, and prostaglandin F2α, and inhibits the proliferation of hepatic stellate cells, formation of stress fibers, and expression of α-SMA, while also repressing cell growth without inducing apoptosis. Fasudil curtails the phosphorylation of ERK1/2, JNK, and p38 MAPK induced by LPA. Additionally, it exerts vasodilatory effects by inhibiting the contraction induced by serotonin, noradrenaline, histamine, angiotensin, and dopamine. |
キナーゼ試験 | Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter. |
別名 | Fasudil (HA-1077) HCl, HA-1077, Fasudil HCl, HA-1077 hydrochloride, AT-877 |
分子量 | 327.83 |
分子式 | C14H18ClN3O2S |
CAS No. | 105628-07-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 32.8 mg/mL (100 mM)
DMSO: 60 mg/mL (183.02 mM)
You can also refer to dose conversion for different animals. 詳細
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Fasudil hydrochloride 105628-07-7 Autophagy Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling Membrane transporter/Ion channel Metabolism Microbiology/Virology Proteases/Proteasome Stem Cells Tyrosine Kinase/Adaptors ROCK Calcium Channel Serine/threonin kinase HIV Protease PKA PKC TWNT-4 cells TIMP-1 HA 1077 a-SMA Protein kinase A Ca channels HIV rat HSCs AT877 Rho-associated protein kinase human HSC ERK1/2 Rho-kinase inhibit Ca2+ channels Rho-associated kinase HA1077 Hydrochloride Fasudil (HA-1077) HCl p38 lysophoaphatidic acid Fasudil Ca2+ channel antagonist JNK HA 1077 Hydrochloride HA-1077 protein kinases collagen LPA HA1077 Inhibitor Fasudil HCl Fasudil Hydrochloride Protein kinase C vasodilator ROK HA-1077 hydrochloride AT 877 Human immunodeficiency virus orally active AT-877 HA-1077 Hydrochloride inhibitor