YS-49 是PI3K/Akt(RhoA 的下游靶标) 的激活剂,可减少 3-甲基胆碱处理的细胞中 RhoA/PTEN 的激活。YS-49 能通过诱导血红素加氧酶 (HO-1) 来抑制血管紧张素 II (Ang II)刺激 VSMC 细胞的增殖。YS-49 是异喹啉化合物生物碱,因能激活心脏β-adrenoceptors而具有强烈的正性肌力作用。
生物活性 | YS-49 is aPI3K/Akt(a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibitsangiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiacβ-adrenoceptors[1][2][3]. |
体外研究 (In Vitro) | YS-49 (1-100 μM; 18 hours; RAVSMC and RAW 264.7 cells) concentration-dependently inhibits the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to lipopolysaccharide (LPS) plus INF-γ, withIC50values of 22 μM and 30 μM, respectively[2]. YS-49 (10-100 μM; 18 hours; RAVSMC and RAW 264.7 cells) suppresses iNOS gene expression induced by LPS and/or cytokines in RAVSMC and RAW 264.7 cells at the transcriptional level[2].
Cell Viability Assay[2] Cell Line: | RAVSMC and RAW 264.7 cells | Concentration: | 10 μΜ, 30 μΜ and 100 μΜ (RAVSMC cells); 1 μΜ, 10 μΜ and 100 μM (RAW 264.7 cells) | Incubation Time: | 18 hours | Result: | Inhibited the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to LPS+INF-γ, withIC50values of 22 and 30 μM, respectively. |
Western Blot Analysis[2] Cell Line: | RAVSMC and RAW 264.7 cells | Concentration: | 10 μΜ, 30 μΜ and 100 μΜ | Incubation Time: | 18 hours | Result: | Concentration-dependently inhibited the expression of iNOS protein induced by LPS plus IFN-γ. |
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体内研究 (In Vivo) | YS-49 (5 mg/kg; intraperitoneal injection; 8 hours; male Sprague Dawley rats) treatment significantly reduces serum NOx levels in LPS-treated rats, the NOx levels reduce from 86 μM to 34 μM[2].
Animal Model: | Male Sprague Dawley rats (250-300 g)[2] | Dosage: | 5 mg/kg | Administration: | Intraperitoneal injection; 8 hours | Result: | Serum NOx levels were significantly reduced. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(258.88 mM;Need ultrasonic) H2O : 10 mg/mL(25.89 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.5888 mL | 12.9440 mL | 25.8880 mL | 5 mM | 0.5178 mL | 2.5888 mL | 5.1776 mL | 10 mM | 0.2589 mL | 1.2944 mL | 2.5888 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 (stored under nitrogen)。-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: 6.67 mg/mL (17.27 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.47 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 (6.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.47 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 (6.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.47 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。 *以上所有助溶剂都可在本网站选购。
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