Propranolol |
| رقم الكتالوجGC36980 |
بروبانولول هو مضاد لمستقبلات بيتا-أدرينالين غير انتقائي (βAR)، وله تفاعل عالٍ مع β1AR و β2AR بقيم Ki قدرها 1.8 نانومتر و 0.8 نانومتر على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 525-66-6
Sample solution is provided at 25 µL, 10mM.
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Propranolol is a non-selective β-adrenergic receptor (βAR) antagonist, exhibiting high affinity for both β1AR and β2AR, with Ki values of 1.8 nM and 0.8 nM, respectively[1]. It inhibits the binding of [3H]-DHA to rat brain membrane preparations with an IC50 of 12 nM[2]. Propranolol is used in research related to hypertension, pheochromocytoma, myocardial infarction, arrhythmias, angina, and hypertrophic cardiomyopathy[3].
In vitro, propranolol increases total ERK1/2 levels in a dose-dependent manner within the concentration range of 10-7 M to 10-3 M, after 24 and 48 hours of treatment, and specifically activates ERK1/2 at a concentration of 10-5 M[4]. After 24 hours of treatment at a concentration of 10-4 M, and after 48 hours at 10-9 M, propranolol significantly reduces the proliferation of HemSC cells[4]. Moreover, propranolol treatment at concentrations ranging from 50µM to 200µM for 24 hours increases the number of Annexin V-positive HemSCs, activates caspase-3, thereby rapidly inducing apoptosis in HemSC cells[4].
In vivo, propranolol (40 mg/kg/d, p.o.) significantly reduces the diameter and blood flow of vessels in an infantile hemangioma (IH) mouse model, while also promoting the activation of ERK1/2 within IH cells[4]. In the Tg2576 Alzheimer's disease transgenic mouse model, propranolol (5mg/kg/d, i.p.) is able to improve cognitive deficits demonstrated in novel object recognition and fear conditioning tests, reduce the increase in Aβ42 levels in the hippocampus, increase in Akt phosphorylation, and excessive phosphorylation of Tau[5].
References:
[1] Galandrin S, et al. Distinct signaling profiles of beta1 and beta2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol Pharmacol. 2006 Nov;70(5):1575-84.
[2] Briley M, et al. Evidence against beta-adrenoceptor blocking activity of diltiazem, a drug with calcium antagonist properties. Br J Pharmacol. 1980 Aug;69(4):669-73.
[3] Al-Majed AA, et al. Propranolol. Profiles Drug Subst Excip Relat Methodol. 2017;42:287-338.
[4] Munabi NC, et al. Propranolol Targets Hemangioma Stem Cells via cAMP and Mitogen-Activated Protein Kinase Regulation. Stem Cells Transl Med. 2016 Jan;5(1):45-55.
[5] Marta D , Gorka G ,RamÍrez MarÍa J. Propranolol reduces cognitive deficits, amyloid and tau pathology in Alzheimer's transgenic mice[J]. Int J Neuropsychopharmacol, 2013(10): 2245-2257.
| Cell experiment [1]: | |
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Cell lines |
LPS and LMS cells |
|
Preparation Method |
cells were treated with 10 µM doxorubicin, 100/150 µM propranolol and their combination. After 4 and 24 h of treatment, the cells were harvested, washed in PBS1X and resuspended in 3% BSA in PBS. To evaluate P-gp membrane expression, the cells were incubated for 30 min at 4 °C with monoclonal anti-P-gp (JSB-1, Abcam) in 3% BSA in PBS. |
|
Reaction Conditions |
100/150 µM; 4/24 h |
|
Applications |
Propranolol inhibited the P-gp-dependent transport of doxorubicin in both LPS and LMS cells and that the higher the expression of P-gp is on the membrane, the stronger the inhibition of doxorubicin efflux by propranolol. |
| Animal experiment [2]: | |
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Animal models |
IH (infantile hemangiomas ) mouse |
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Preparation Method |
Propranolol was diluted to 270 µM in 5% dextrose water (vehicle), and daily consumption was measured to calculate the treatment dosage, which averaged 40 mg/kg daily. The mice were sacrificed after 21 days. |
|
Dosage form |
40 mg/kg/d; 21 days; p.o. |
|
Applications |
Propranolol significantly reduces the diameter and blood flow of vessels in an infantile hemangioma (IH) mouse model, while also promoting the activation of ERK1/2 within IH cells. |
|
References: [1] Porcelli L , Garofoli M , Fonte R D ,et al. The β-adrenergic receptor antagonist propranolol offsets resistance mechanisms to chemotherapeutics in diverse sarcoma subtypes: a pilot study[J].Scientific Reports, 2020, 10(1). |
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| Cas No. | 525-66-6 | SDF | |
| Canonical SMILES | OC(COC1=C2C=CC=CC2=CC=C1)CNC(C)C | ||
| Formula | C16H21NO2 | M.Wt | 259.34 |
| الذوبان | DMSO : 100 mg/mL (385.59 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8559 mL | 19.2797 mL | 38.5594 mL |
| 5 mM | 771.2 μL | 3.8559 mL | 7.7119 mL |
| 10 mM | 385.6 μL | 1.928 mL | 3.8559 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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