Y-27632 dihydrochloride 是一种具有口服活性的、ATP 竞争性的ROCK(Rho-kinase) 抑制剂 (ROCK-IKi=220 nM; ROCK-IIKi=300 nM)。Y-27632 dihydrochloride 表现出抗癫痫的作用。
生物活性 | Y-27632 dihydrochloride is an orally active and ATP-competitiveROCK(Rho-kinase) inhibitor (ROCK-IKi=220 nM; ROCK-IIKi=300 nM). Y-27632 dihydrochloride shows antiepileptic effects[1][2][3][4]. |
IC50& Target[1] | ROCK-I 220 nM (Ki) | ROCK-II 300 nM (Ki) | PKN 3.1 μM (Ki) | Citron kinase 5.3 μM (Ki) | PKCα 73 μM (Ki) | PKA 25 μM (Ki) |
|
体外研究 (In Vitro) | Y-27632 (1-5 μM; 0-60 min) promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs)[3]. Y-27632 (1-5 μM; 0-60 min) induces the expression of NSE, MAP-2 and nestin in ADSCs[3].
Western Blot Analysis[3] Cell Line: | Adipose tissue-derived stem cells (ADSCs) | Concentration: | 20 μM | Incubation Time: | 24 hours | Result: | Resulted in the up-regulation of NSE, MAP-2 and nestin protein levels by 25.3, 3.1 and 2.5 fold, respectively, compared to control cells not treated by Y-27632. |
|
体内研究 (In Vivo) | Y-27632 (oral gavage; 30 mg/kg; once daily; 4 w) prevents dimethylnitrosamine-induced hepatic fibrosis in rats[1]. Y-27632 (oral gavage; 5-10 mg/kg; once) shows antiepileptic effects in epilepsy induced by PTZ and MES[2].
Animal Model: | Male Wistar rats injected with dimethylnitrosamine[1] | Dosage: | 30 mg/kg | Administration: | Oral gavage; 30 mg/kg; once daily; 4 weeks | Result: | Decreased the occurrence of dimethylnitrosamine-induced hepatic fibrosis and reduced the collagen and hydroxyproline content and α-smooth muscle actin expression in the liver. |
Animal Model: | Male Swiss albino mice injected with PTZ (pentylenetetrazole) or induced by MES (maximal electroconvulsive shock)[2] | Dosage: | 5-10 mg/kg | Administration: | Oral gavage; 5-10 mg/kg; once | Result: | Prolonged the onset time of myoclonic jerks when compared with those observed in the saline group (P<0.05). Prolonged the onset time of clonic convulsions when compared with saline group (P<0.05). Prevented the occurrence of tonic hindlimb extensions and death. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(312.25 mM;Need ultrasonic) DMSO : 33.33 mg/mL(104.07 mM;Need ultrasonic) 配制储备液 1 mM | 3.1225 mL | 15.6123 mL | 31.2246 mL | 5 mM | 0.6245 mL | 3.1225 mL | 6.2449 mL | 10 mM | 0.3122 mL | 1.5612 mL | 3.1225 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 220 mg/mL (686.94 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.81 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.81 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.81 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 5. 请依序添加每种溶剂: 5% DMSO 40%PEG300 5%Tween-80 50% saline Solubility: ≥ 1.25 mg/mL (3.90 mM); Clear solution 6. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (3.90 mM); Clear solution *以上所有助溶剂都可在本网站选购。
|