| 名稱(chēng) | Fasudil hydrochloride |
| 描述 | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 靜脈注射0.01,0.03,0.1 和 0.3 mg/kg Fasudil劑量依賴(lài)性地降低MBP,提高HR,VBF,CBF,RBF和FBF.總劑量為1.0 ng/mL的 Fasudil提高心臟的輸出量.通過(guò)冠狀動(dòng)脈內(nèi)注射給實(shí)驗(yàn)狗30 μg Fasudil導(dǎo)致CBF增加約50％.口服Fasudil（劑量為100 mg/kg/天）顯著降低用PLP p139-151免疫的SJL/J小鼠中EAE的發(fā)病率和平均最大臨床評(píng)分.Fasudil抑制小鼠脾細(xì)胞對(duì)抗原的增殖反應(yīng).Fasudil處理顯示心血管疾病的保護(hù)作用,并減少JNK的激活和減少AIF在缺血性損傷下的線粒體核移位. |
| 體內(nèi)活性 | Fasudil誘導(dǎo)肌動(dòng)蛋白纖維解體,且抑制細(xì)胞遷移。Fasudil競(jìng)爭(zhēng)性抑制Ca2+誘導(dǎo)的去極化兔主動(dòng)脈收縮。Fasudil抑制對(duì)KCl,血清苯丙氨酸和前列腺素F2a的收縮反應(yīng)。Fasudil抑制肝星狀細(xì)胞的擴(kuò)散,應(yīng)力纖維的形成和α-SMA的表達(dá),且抑制細(xì)胞生長(zhǎng),但不誘導(dǎo)細(xì)胞凋亡。Fasudil抑制LPA誘導(dǎo)的ERK1/2,JNK 和 p38 MAPK磷酸化。Fasudil還通過(guò)抑制5-羥色胺,去甲腎上腺素,組胺,血管緊張素和多巴胺誘導(dǎo)的螺旋條收縮來(lái)發(fā)揮血管舒張作用。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 32.8 mg/mL (100 mM)
DMSO : 60 mg/mL (183.02 mM)
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| 關(guān)鍵字 | Fasudil hydrochloride | TWNT-4 cells | TIMP-1 | HA 1077 | a-SMA | Protein kinase A | Ca channels | PKA | HIV | rat HSCs | AT877 | Rho-associated protein kinase | human HSC | ERK1/2 | Rho-kinase | inhibit | PKC | Ca2+ channels | Rho-associated kinase | HA1077 Hydrochloride | p38 | lysophoaphatidic acid | Fasudil | Ca2+ channel antagonist | JNK | HA 1077 Hydrochloride | Calcium Channel | protein kinases | collagen | LPA | HA1077 | ROCK | Inhibitor | Fasudil Hydrochloride | Protein kinase C | vasodilator | ROK | AT 877 | Human immunodeficiency virus | Autophagy | orally active | HA-1077 Hydrochloride |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Emtricitabine | Hydroxychloroquine | Lamivudine |
| 相關(guān)庫(kù) | 神經(jīng)保護(hù)化合物庫(kù) | 抗癌上市藥物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 離子通道庫(kù) | 膜蛋白靶向化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 抗癌藥物庫(kù) |