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Pronetalol

Cat No.:V5566 Purity: ≥98%
Pronethalol ((±)-Pronethalo) is a non-selective beta-adrenergic antagonist.
Pronetalol
Pronetalol Chemical Structure CAS No.: 54-80-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
100mg
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Other Forms of Pronetalol:

  • Pronetalol hydrochloride
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Pronethalol ((±)-Pronethalo) is a non-selective beta-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol prevents and reverses digitalis-induced ventricular arrhythmias and may also limit cerebral arteriovenous malformations (AVMs).
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In ReNcell VM cells, pronethalol (2, 10, 20 μM) suppresses EGFP expression in a time- and dose-dependent manner. After two days of treatment, Sox2 expression is reduced to less than 10% by pronethalol (10 μM; two days) [2].
ln Vivo
In Mgp-/-mice, pronethalol (0.15 mg/g; daily; for 14 days) improves cerebral arteriovenous malformations (AVMs) and stabilizes endothelial differentiation and lumen formation [2].
References

[1]. The effects of a beta-adrenergic blocking agent, pronethalol, on digitalis-induced ventricular arrhythmias. Am Heart J. 1966 Apr;71(4):503-8.

[2]. Elevated endothelial Sox2 causes lumen disruption and cerebral arteriovenous malformations. J Clin Invest. 2019 Jun 24;129(8):3121-3133.

[3]. The effects of a beta-adrenergic blocking agent, pronethalol, on digitalis-induced ventricular arrhythmias. Am Heart J. 1966 Apr;71(4):503-508.

Additional Infomation
Pronethalol is a member of naphthalenes.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H19NO
Molecular Weight
229.31746
Exact Mass
229.147
CAS #
54-80-8
Related CAS #
Pronethalol hydrochloride;51-02-5
PubChem CID
4930
Appearance
White to off-white solid powder
Density
1.074g/cm3
Boiling Point
322.4ºC at 760mmHg
Flash Point
84.3ºC
LogP
3.262
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
4
Heavy Atom Count
17
Complexity
229
Defined Atom Stereocenter Count
0
InChi Key
HRSANNODOVBCST-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H19NO/c1-11(2)16-10-15(17)14-8-7-12-5-3-4-6-13(12)9-14/h3-9,11,15-17H,10H2,1-2H3
Chemical Name
1-naphthalen-2-yl-2-(propan-2-ylamino)ethanol
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~218.04 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (10.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.3607 mL 21.8036 mL 43.6072 mL
5 mM 0.8721 mL 4.3607 mL 8.7214 mL
10 mM 0.4361 mL 2.1804 mL 4.3607 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • A high-throughput system identifies pronethalol as an inhibitor of Sox2 expression. (A) Schematic diagram of the high-throughput system used for screening candidate compounds that may suppress Sox2 expression in ReNcell VM cells. (B and C) Expression of EGFP in ReNcell VM cells after treatment with increasing doses of pronethalol, as (B) detected by fluorescence microscope and (C) quantitated by ImageJ software (n = 5). Scale bars: 50 μm. (D) Time-course expression of EGFP in ReNcell VM cells treated with 10 μM pronethalol (n = 5). (E and F) Dose and time-course expression of Sox2 after treatment with pronethalol in ReNcell VM cells (n = 5). (G) Decreased expression of Sox2, JMJD5, N-cadherin, Par3, and Rasip1 in MGP CRISPR cells after treatment with 10 μM pronethalol for 48 hours, as shown by immunoblotting (n = 5). (H–J) Expression of (H) β1-, (I) β2- or (J) β3-adrenergic receptors (β1, β2, and β3) in ReNcell VM cells transfected with siRNA to individual β1-, β2-, or β3-adrenergic receptors (β1 si, β2 si, and β3 si) (n = 5). SCR, scrambled siRNA. (K) Expression of Sox2 in ReNcell VM cells treated with pronethalol and transfected with siRNA to individual β1-, β2-, or β3-adrenergic receptors (n = 5). SCR, scrambled siRNA. (L–N) Expression of (L) β1-, (M) β2-, or (N) β3-adrenergic receptors in MGP CRISPR cells transfected with siRNA to individual β1-, β2-, or β3-adrenergic receptors (n = 5). (O) Expression of Sox2 in MGP CRISPR cells treated and transfected with siRNA to individual β1-, β2-, or β3-adrenergic receptors (n = 5). Data shown in H–J and L–N were analyzed by Student’s t test. Data shown in E, F, K, and O were analyzed by 1-way ANOVA with Tukey’s multiple comparisons test. Data are shown by box and whisker plots. The bounds of the boxes represent upper and lower quartiles. The lines in the boxes represent the median, and the whiskers represent the maximum and minimal values. ***P < 0.001.[2]. Jiayi Yao, et al. Elevated endothelial Sox2 causes lumen disruption and cerebral arteriovenous malformations. J Clin Invest. 2019 Jun 24;129(8):3121-3133.
  • Pronethalol improves cerebral AVMs in Mgp–/– mice. (A) Pronethalol decreases arteriovenous shunting in Mgp–/– mice, as demonstrated by UV-fluorescent microsphere injections (n = 5). Scale bars: 1 mm. (B) Relative density of retained fluorescent microspheres in the brains of Mgp+/+ and Mgp–/– mice after treatment with pronethalol (n = 5). (C) μCT images of the cerebral vasculature with colors reflecting the vessel radii from Mgp+/+ and Mgp–/– mice with or without treatment with pronethalol (n = 3). Scale bars: 1 mm. (D) Frequency of vessels with different radii in the cerebra of mice detected by μCT imaging (n = 3). (E) Expression of Sox2, JMJD5, N-cadherin, and Par3 in cerebral ECs isolated from Mgp+/+ and Mgp–/– mice that were treated with pronethalol (n = 6). (F and G) Arteriovenous shunting examined by UV-fluorescent microsphere passage in lungs and kidneys (n = 4). Data shown in B and E were analyzed by 1-way ANOVA with Tukey’s multiple comparisons test. Data are shown by box and whisker plots. The bounds of the boxes represent upper and lower quartiles. The lines in the boxes represent the median, and the whiskers represent the maximum and minimal values. ***P < 0.001.[2]. Jiayi Yao, et al. Elevated endothelial Sox2 causes lumen disruption and cerebral arteriovenous malformations. J Clin Invest. 2019 Jun 24;129(8):3121-3133.
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