Propranolol 是一种非选择性的β-adrenergic receptor (βAR)拮抗剂,对 β1AR 和 β2AR 具有高亲和力,Ki值分别为 1.8 nM 和 0.8 nM。Propranolol 抑制[3H]-DHA 与大鼠脑膜制剂的结合,IC50为 12 nM。Propranolol 用于高血压,嗜铬细胞瘤,心肌梗塞,心律不齐,心绞痛和肥大心肌病的相关研究。
生物活性 | Propranolol is a nonselectiveβ-adrenergic receptor (βAR)antagonist, has high affinity for the β1AR and β2AR withKivalues of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with anIC50of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3]. |
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体外研究 (In Vitro) | Propranolol (10-7M-10-3M; 24 and 48 hours) increases the total ERK1/2 levels in a dose-dependent manner, and ERK1/2 activation is observed specifically at 10-5M in HemSCs[4].Propranolol (10-9M-10-3M; 24 and 48 hours) significant decreases cell proliferation at 10-4M propranolol after 24 hours and 10-9M propranolol after 48 hours in HemSCs[4].Propranolol (50 μM-200 μM;24 hours) increases Annexin V positivity and caspase-3 activation, rapidly induces HemSC apoptosis[4].
Western Blot Analysis[4] Cell Line: | HemSC cells | Concentration: | 10-7M-10-3M | Incubation Time: | 24 and 48 hours | Result: | Increased the total ERK1/2 levels in a dose-dependent manner. |
Cell Proliferation Assay[4] Cell Line: | HemSC cells | Concentration: | 10-9M-10-3M | Incubation Time: | 24 and 48 hours | Result: | Suppressed HemSC proliferation. |
Apoptosis Analysis[4] Cell Line: | HemSC cells | Concentration: | 50 μM, 100 μM, or 200 μM | Incubation Time: | 24 hours | Result: | Induced HemSC cell death occurred via an apoptotic pathway. |
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体内研究 (In Vivo) | Propranolol (orally administration; 40 mg/kg; daily) significantly reduces the vessel diameter relative to the vehicle-treated implants, and increases the number of cells that expressed phosphorylated ERK1/2 within the IH Matrigel implant[4].
Animal Model: | A xenograft mouse model of IH (infantile hemangiomas ) with HemSC cells[4] | Dosage: | 40 mg/kg | Administration: | Orally administration; 40 mg/kg; daily | Result: | Improved vessel development in the IH mouse model that correlated with MAPK pathway activation. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(385.59 mM;Need ultrasonic) 配制储备液 1 mM | 3.8559 mL | 19.2797 mL | 38.5594 mL | 5 mM | 0.7712 mL | 3.8559 mL | 7.7119 mL | 10 mM | 0.3856 mL | 1.9280 mL | 3.8559 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。-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: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.64 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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