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| 100mg |
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| 250mg |
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| 1g |
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Purity: ≥98%
Amiloride HCl (MK-870; Midamor; Midoride; Modamide), the hydrochloride salt of amiloride, is a potent and relatively selective inhibitor of the epithelial sodium channel (ENaC) with anti-hypertensive activity. It was first approved in 1967 for use in the management of hypertension and congestive heart failure. Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene).
| ln Vitro |
Amiloride has an IC50 of 2.6 μM and blocks δβγ channels. In comparison to αβγ channels (0.1 μM for αβγ ENaC), amiloride hydrochloride's Ki for δΗη ENaC is 26 times greater. Amiloride hydrochloride more strongly depends on voltage to block δβγ ENaC than it does αβγ channels. In accordance with the K of the αβη and δβγ channels [1], the Ki of amiloride hydrochloride for the δαβγ channels are 920 and 13.7 μM at -120 and +80 mV, respectively. With an IC50 (concentration needed to achieve 50% inhibition of the ion channel) in the concentration range of 0.1 to 0.5 μM, amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC). With an IC50 as low as 3 μM in the presence of low external [Na+] and as high as 1 mM in the presence of high [Na+], amiloride is a relatively poor inhibitor of Na+/H+ exchangers (NHE). Amiloride has an IC50 of 1 mM, making it a weaker inhibitor of the Na+/Ca2+ exchanger (NCX). By inhibiting the activity of the ENaC protein, amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), which are known to inhibit ENaC, prevent the myogenic vasoconstriction response to elevated perfusion pressure. In vascular smooth muscle cells (VSMC), amiloride completely inhibits Na+ influx at a dose that is known to be relatively specific for ENaC (1.5 μM) [2].
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| ln Vivo |
It was discovered that giving DOCA salt hypertensive rats a subcutaneous injection of amiloride (1 mg/kg/day) will reverse the initial rise in collagen deposition and stop any additional increases. In stroke-prone, saline-drinking spontaneously hypertensive rats (SHRSP), amiloride improved kidney and brain histology scores and postponed the onset of proteinuria as compared to controls. In animals with salt-dependent hypertension, amiloride hydrochloride counteracts or inhibits the effects of aldosterone in these cells as well as in the cardiovascular and renal organs [2].
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| References |
[1]. Ji, H.L., et al. delta ENaC: a novel divergent amiloride-inhibitable sodium channel. Am J Physiol Lung Cell Mol Physiol, 2012. 303(12): p. L1013-26.
[2]. Teiwes J, et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. [3]. Giamarchi A, et al. A polycystin-2 (TRPP2) dimerization domain essential for the function of heteromeric polycystin complexes. EMBO J. 2010 Apr 7;29(7):1176-91. |
| Molecular Formula |
C6H8CLN7O.HCL
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| Molecular Weight |
266.09
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| CAS # |
2016-88-8
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| Related CAS # |
Amiloride hydrochloride dihydrate;17440-83-4;Amiloride;2609-46-3;Amiloride hydrochloride (Standard);2016-88-8;Amiloride-15N3 hydrochloride;1216796-18-7
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| SMILES |
N=C(NC(=O)C1C(N)=NC(=C(N=1)Cl)N)N.Cl
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| InChi Key |
ACHKKGDWZVCSNH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H8ClN7O.ClH/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11;/h(H4,8,9,13)(H4,10,11,14,15);1H
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| Chemical Name |
3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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: ≥ 2.5 mg/mL (9.40 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 (9.40 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 (9.40 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 | 3.7581 mL | 18.7906 mL | 37.5813 mL | |
| 5 mM | 0.7516 mL | 3.7581 mL | 7.5163 mL | |
| 10 mM | 0.3758 mL | 1.8791 mL | 3.7581 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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