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) |
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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. |
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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. |
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| 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。
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