Amlodipine besylate (Amlodipine benzenesulfonate) 是一种抗心绞痛剂和具有口服活性二氢吡啶钙通道阻滞剂,通过阻断电压依赖性的 L 型钙通道,从而抑制钙离子内流。Amlodipine besylate 可用于高血压和癌症的研究。
生物活性 | Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridinecalcium channelblocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure andcancer[1][2][3]. |
IC50& Target | L-type calcium channel[1] |
体外研究 (In Vitro) | Amlodipine besylate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3]. Amlodipine besylate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]iin A431 cells[3]. Amlodipine besylate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].
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体内研究 (In Vivo) | Amlodipine besylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMCATP2B1KO mice[4]. Amlodipine besylate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].
Animal Model: | ATP2B1loxP/loxPmice[4] | Dosage: | 5 mg/kg/day | Administration: | Subcutaneously implanted osmotic pump for 2 weeks | Result: | Significantly decreased the blood pressure. |
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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: DMSO : ≥ 45 mg/mL(79.36 mM) H2O : 1 mg/mL(1.76 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 1.7635 mL | 8.8176 mL | 17.6351 mL | 5 mM | 0.3527 mL | 1.7635 mL | 3.5270 mL | 10 mM | 0.1764 mL | 0.8818 mL | 1.7635 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: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.41 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 (4.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.41 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 (4.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.41 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。 4. 请依序添加每种溶剂: PBS Solubility: 2 mg/mL (3.53 mM); Clear solution; Need ultrasonic *以上所有助溶剂都可在本网站选购。
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