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| 25g |
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Purity: ≥98%
Hexamethonium Bromide (Vegolysen; Esametina; Simpatoblock), a peripherally-acting and nondepolarizing neuromuscular blocker, is a selective antagonist of neuronal-type nicotinic AChR in ganglia that was used to treat chronic hypertension. But the use of Hexamethonium was discontinued due to the non-specificity of its action.
| ln Vitro |
The depolarization of smooth muscle cells caused by epibatidine is eliminated by hexamethonium bromide (100 µM; 60 minutes)[1]. When exposed to Hexamethonium Bromide, the α3β4α5 receptors are more sensitive than the other possible ganglionic models, α3β4, α3β2, and α3β2α5[2].
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| ln Vivo |
In both Wistar and spontaneously hypertensive rats (SHRs), hexamethonium bromide (0.2–25 mg/kg; iv) dramatically lowers heart rate (HR), mean arterial pressure (MAP), and renal sympathetic nerve activity (RSNA)[4]. Between Wistar rats and SHRs, hexamethonium bromide (0.2-1.0 mg/kg; iv) treatments do not significantly alter the RSNA, MAP, or HR[4]. In comparison to Wistar rats, SHRs experience a higher decrease in the RSNA and MAP when exposed to hexamethonium bromide (5.0–25 mg/kg; iv)[4].
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| Animal Protocol |
Animal/Disease Models: Male normotensive Wistar rats (280-320 g), SHRs[4]
Doses: 0.2 mg/kg, 1.0 mg/kg, 5.0 mg/kg , 25 mg/kg Route of Administration: intravenous (iv) injection Experimental Results: Dramatically decreased the RSNA, MAP and HR in the Wistar rats and the SHRs. |
| References |
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| Additional Infomation |
A nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. It has been used for a variety of therapeutic purposes including hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool.
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| Molecular Formula |
C12H30N2.2BR
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|---|---|---|
| Molecular Weight |
362.19
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| Exact Mass |
360.077
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| CAS # |
55-97-0
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| Related CAS # |
Hexamethonium chloride;60-25-3
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| PubChem CID |
5938
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| Appearance |
White to off-white solid powder
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| Melting Point |
~285 °C (dec.)
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
16
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| Complexity |
121
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FAPSXSAPXXJTOU-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C12H30N2.2BrH/c1-13(2,3)11-9-7-8-10-12-14(4,5)6;;/h7-12H2,1-6H3;2*1H/q+2;;/p-2
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| Chemical Name |
N1,N1,N1,N6,N6,N6-hexamethylhexane-1,6-diaminium bromide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.61 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 16.7 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: ≥ 1.67 mg/mL (4.61 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 16.7 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. View More
Solubility in Formulation 3: 100 mg/mL (276.10 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7610 mL | 13.8049 mL | 27.6098 mL | |
| 5 mM | 0.5522 mL | 2.7610 mL | 5.5220 mL | |
| 10 mM | 0.2761 mL | 1.3805 mL | 2.7610 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.
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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