Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Benzamil HCl, the hydrochloride salt of Benzamil which is an amiloride analog, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM) with the potential to treat cystic fibrosis. Benzamil is also a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM.
ln Vitro |
Small conductance Ca2+-activated K2+ channels in neurons and heterologously generated K2+ channels are inhibited by benamil hydrochloride (benzylamiloride hydrochloride) [4].
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ln Vivo |
After receiving Benzamil hydrochloride treatment (0.7 mg/kg/day; sc), stroke-prone spontaneously hypertensive rats (SHRSP) lived an average of 16.1 weeks [5].
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References |
[1]. Fischer KG, et al. Characterization of a Na(+)-Ca(2+) exchanger in podocytes. Nephrol Dial Transplant. 2002 Oct;17(10):1742-50.
[2]. Wang X, et al. Effects of amiloride, benzamil, and alterations in extracellular Na+ on the rat afferent arteriole and its myogenic response. Am J Physiol Renal Physiol. 2008 Jul;295(1):F272-82. [3]. Dai XQ, et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85. [4]. Castañeda MS, et al. Benzamil inhibits neuronal and heterologously expressed small conductance Ca2+-activated K+channels. Neuropharmacology. 2019 Nov 1;158:107738. [5]. Teiwes J, et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-1 |
Molecular Formula |
C13H15CL2N7O
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Molecular Weight |
356.2105
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CAS # |
161804-20-2
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Related CAS # |
Benzamil;2898-76-2
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SMILES |
ClC1C(N([H])[H])=NC(=C(C(N([H])/C(/N([H])[H])=N/C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=O)N=1)N([H])[H].Cl[H]
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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)
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Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~280.73 mM)
H2O : ~1 mg/mL (~2.81 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.02 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 (7.02 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8073 mL | 14.0367 mL | 28.0733 mL | |
5 mM | 0.5615 mL | 2.8073 mL | 5.6147 mL | |
10 mM | 0.2807 mL | 1.4037 mL | 2.8073 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.