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Bretylium tosylate

Cat No.:V17018 Purity: ≥98%
Bretylium (tosylate) is an inhibitor (blocker/antagonist) of presynaptic release of vasoconstrictive neurotransmitters and a blocker of sympathetic and adrenergic nerves.
Bretylium tosylate
Bretylium tosylate Chemical Structure CAS No.: 61-75-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Bretylium (tosylate) is an inhibitor (blocker/antagonist) of presynaptic release of vasoconstrictive neurotransmitters and a blocker of sympathetic and adrenergic nerves.
Biological Activity I Assay Protocols (From Reference)
References

[1]. Adenosine receptor inhibition attenuates the suppression of postexercise cutaneous blood flow. J Physiol. 2014 Jun 15;592(12):2667-78.

[2]. Aging and aerobic fitness affect the contribution of noradrenergic sympathetic nerves to the rapid cutaneous vasodilator response to local heating. J Appl Physiol (1985). 2011 May;110(5):1264-70.

[3]. Leptin inhibits gastric emptying in rats: role of CCK receptors and vagal afferent fibers. Physiol Res. 2007;56(3):315-22. Epub 2006 Jun 22.

Additional Infomation
Bretylium tosylate is the tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. It has a role as an adrenergic antagonist, an anti-arrhythmia drug and an antihypertensive agent. It is a quaternary ammonium salt and an organosulfonate salt. It contains a bretylium.
Bretylium Tosylate is the tosylate salt form of bretylium, a quaternary ammonium salt and non-selective adrenergic neuronal blocking agent with anti-arrhythmic properties. Bretylium tosylate is selectively taken up into peripheral nerve terminals and initially causes a release of norepinephrine from sympathetic nerve endings, thereby causing a sympathomimetic effect. This is followed by a prolonged anti-adrenergic action which prevents further discharge of neurotransmitter from sympathetic nerve endings. Its myocardial effects include a prolongation of action potential as well as refractory period. This drug is used to treat and suppress ventricular arrhythmias, particularly ventricular fibrillation and ventricular tachycardia.
An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H24BRNO3S
Molecular Weight
414.3571
Exact Mass
413.066
CAS #
61-75-6
PubChem CID
6100
Appearance
White to off-white solid powder
Melting Point
97-99°
LogP
5.025
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
3
Heavy Atom Count
24
Complexity
349
Defined Atom Stereocenter Count
0
InChi Key
KVWNWTZZBKCOPM-UHFFFAOYSA-M
InChi Code
InChI=1S/C11H17BrN.C7H8O3S/c1-4-13(2,3)9-10-7-5-6-8-11(10)12;1-6-2-4-7(5-3-6)11(8,9)10/h5-8H,4,9H2,1-3H3;2-5H,1H3,(H,8,9,10)/q+1;/p-1
Chemical Name
(2-bromophenyl)methyl-ethyl-dimethylazanium;4-methylbenzenesulfonate
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

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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 : ~100 mg/mL (~241.34 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (6.03 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 (6.03 mM) 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; with ultrasonication.
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 (6.03 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.
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 2.4134 mL 12.0668 mL 24.1336 mL
5 mM 0.4827 mL 2.4134 mL 4.8267 mL
10 mM 0.2413 mL 1.2067 mL 2.4134 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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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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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

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