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Isoprenaline hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Isoprenaline hydrochloride图片
CAS NO:51-30-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
200mg电议
1 g电议
5 g电议
10 g电议

产品名称
盐酸异丙肾上腺素
Isoproterenol hydrochloride
产品介绍
Isoprenaline (Isoproterenol) hydrochloride 是一种非选择性的 β-肾上腺素受体激动剂,具有口服活性。Isoprenaline 具有强效的外周血管扩张、支气管扩张和心脏刺激活性。Isoprenaline 可用于心动过缓和支气管哮喘的研究。
生物活性

Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally activeβ-adrenergic receptoragonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma[1][2][3][4][5][6].

IC50& Target

β adrenergic receptor

 

体外研究
(In Vitro)

Isoprenaline (Isoproterenol) hydrochloride (300 nM, 3 min) increases particulate cGMP- and cilostamide-inhibited, low-KmcAMP phosphodiesterase (cAMP-PDE) activity by about 100% in intact rat fat cells[1].
Isoprenaline inhibits insulin-stimulated glucose transport activity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approximately 2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of >50%, which directly correlated with the observed inhibition of transport activity[2].
Isoprenaline (5 nM and 10 μM) increases cyclic AMP levels and this effect is potentiated by cilostamide (10 mM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO)[3].
Isoprenaline increases the transcriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gs alpha remains unchanged[4].
Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift of approximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+current[5].
Isoprenaline (20 nM) increases the spontaneous pacemaker rate of sino-atrial node pacemaker cells by 16% in rabbit isolated pacemaker cells[5].

体内研究
(In Vivo)

Isoprenaline (Isoproterenol) hydrochloride (oral, 0.27-0. 64 μg/kg) is extensively metabolizes by a relatively small number of reactions in dogs[6].

Animal Model:Dogs[1]
Dosage:0.27-0. 64 μg/kg
Administration:oral
Result:Excreted largely unchanged in urine, only one-third of the radioactivity in urine was in the form of the O-methyl metabolite.
Showed plasma radioactivity was almost entirely as conjugated isoprenaline and this metabolite accounted for more than 80% of radioactivity in urine.
. Showed heart rate returned to base-line values when high plasma concentrations.
Clinical Trial
分子量

247.72

性状

Solid

Formula

C11H18ClNO3

CAS 号

51-30-9

中文名称

盐酸异丙肾上腺素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 80 mg/mL(322.95 mM;Need ultrasonic)

H2O : ≥ 50 mg/mL(201.84 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.0368 mL20.1841 mL40.3682 mL
5 mM0.8074 mL4.0368 mL8.0736 mL
10 mM0.4037 mL2.0184 mL4.0368 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 and light)。-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: 100 mg/mL (403.68 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: ≥ 2.08 mg/mL (8.40 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (8.40 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (8.40 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.40 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 20.8 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。