Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Isoprenaline hydrochloride (NCI-c55630) 是非选择性的β-肾上腺素能受体激动剂,有支气管扩张剂,外周血管扩张剂和心脏刺激活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
200 mg | ¥ 291 | 现货 | ||
1 g | ¥ 460 | 现货 | ||
5 g | ¥ 1,389 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 418 | 现货 |
产品描述 | Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties. |
体外活性 | 用 Isoprenaline (300 nM,3 分钟)诱导完整的大鼠脂肪细胞,可使微粒 cGMP 和西洛他胺抑制的低 Km cAMP 磷酸二酯酶(cAMP-PDE)活性分别提高约 50%和 100%[1]。环 GMP PDE(PDE 3)抑制剂西洛他胺(100 nM)可增强 Isoprenaline 诱导的松弛。 Isoprenaline (5 nM 和 10 microM)可增加环 AMP 水平,西洛他胺(10 microM)、环 AMP PDE(PDE 4)抑制剂罗利普仑(10 microM)和环 GMP 诱导剂(50 nM ANF 或 30 nM SNP 加 100 nM DMPPO)可增强这种效应[2]。 Isoprenaline 增加了 Akt 以及下游 FoxO1、FoxO3a 和 CREB 的磷酸化水平。当儿茶酚胺与β肾上腺素受体结合时,G蛋白偶联受体激酶-2(GRK2)介导PI3K向β肾上腺素受体转位,然后增强β-arrestin和AP-2的招募,最终导致β肾上腺素受体的内化和下调。有报道称,通过置换 I 类 PI3K 同工酶来破坏 PI3K 和 GRK2 之间的相互作用可阻止激动剂刺激的 β 肾上腺素受体内化 [3]。 |
细胞实验 | Cells are seeded in 24-well culture dishes at a density of 2 to 5×10^4 cells per well. Experiments are performed after 3 to 5 days in culture when cells has reached confluence. Culture medium is aspirated and replaced by 0.5 mL of PBS containing the pharmacological agents. Treatments are performed in quadruplicate at 37°C. The type 3, 4 and 5 PDE inhibitors cilostamide (10 gM), rolipram (10 pM) and DMPPO (10 gM), respectively, are incubated with cells for 30 min before addition of adenylate or guanylate cyclase activators. Cyclic GMP and cyclic AMP are respectively increased in RASMC by stimulation of particulate guanylate cyclase with ANF (50 nM for 10 min) or fl-adrenoceptors with isoprenaline (5 nm for 5 min). At the end of the incubation period, the medium is removed and intracellular cyclic nucleotides are extracted by two ethanolic (65%) ishes at 4°C for 5 min. Ethanolic extracts are pooled, evaporated to dryness by a Speed-Vac system. The dried extract is dissolved in a suitable amount of assay buffer and cyclic nucleotide levels are measured by scintillation proximity assay [3]. |
别名 | NCI-c55630, Isoproterenol hydrochloride, Isoprenaline HCl, 盐酸异丙肾上腺素 |
分子量 | 247.719 |
分子式 | C11H18ClNO3 |
CAS No. | 51-30-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 201.8 mM
DMSO: 201.8 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 4.0368 mL | 20.1842 mL | 40.3683 mL | 100.9208 mL |
5 mM | 0.8074 mL | 4.0368 mL | 8.0737 mL | 20.1842 mL | |
10 mM | 0.4037 mL | 2.0184 mL | 4.0368 mL | 10.0921 mL | |
20 mM | 0.2018 mL | 1.0092 mL | 2.0184 mL | 5.046 mL | |
50 mM | 0.0807 mL | 0.4037 mL | 0.8074 mL | 2.0184 mL | |
100 mM | 0.0404 mL | 0.2018 mL | 0.4037 mL | 1.0092 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Isoprenaline hydrochloride 51-30-9 GPCR/G Protein Metabolism Neuroscience PI3K/Akt/mTOR signaling PI3K Adrenergic Receptor Endogenous Metabolite PDE peripheral vasodilator Isoprenaline NCI-c55630 Beta Receptor cardiac stimulating activities Inhibitor Isoproterenol Isoproterenol hydrochloride Isoprenaline Hydrochloride inhibit bronchodilator Isoprenaline HCl 盐酸异丙肾上腺素 Isoproterenol Hydrochloride inhibitor