Amiloride HCl

Catalog No.S1811 Batch:S181102

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Technical Data

Formula

C6H8ClN7O.HCl
Molecular Weight 266.09 CAS No. 2016-88-8
Solubility (25°C)* In vitro DMSO 53 mg/mL (199.18 mM)
Water 11 mg/mL (41.33 mM)
Ethanol 3 mg/mL (11.27 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 52 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.44mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Targets
Sodium channel [1] T-type calcium channel [2] uPA [3]
7 μM(Ki)
In vitro

Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC). [1]
In vivo

Amiloride at 1 mg/kg/day subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP). compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension. [1]

Protocol (from reference)

Selleck's Amiloride HCl has been cited by 26 publications

Proton pump inhibitors enhance macropinocytosis-mediated extracellular vesicle endocytosis by inducing membrane v-ATPase assembly [ J Extracell Vesicles, 2024, 13(4):e12426] PubMed: 38532609
Proton pump inhibitors enhance macropinocytosis-mediated extracellular vesicle endocytosis by inducing membrane v-ATPase assembly [ J Extracell Vesicles, 2024, 13(4):e12426] PubMed: 38532609
Tetrandrine (TET) inhibits African swine fever virus entry into cells by blocking the PI3K/Akt pathway [ Virus Res, 2024, 339:199258] PubMed: 37923171
Rescue of alveolar wall liquid secretion blocks fatal lung injury due to influenza-staphylococcal coinfection [ J Clin Invest, 2023, 10.1172/JCI163402] PubMed: 37581936
Rescue of alveolar wall liquid secretion blocks fatal lung injury due to influenza-staphylococcal coinfection [ J Clin Invest, 2023, 133(19)e163402] PubMed: 37581936
Real-Time Dissection of the Transportation and miRNA-Release Dynamics of Small Extracellular Vesicles [ Adv Sci (Weinh), 2023, 10(7):e2205566] PubMed: 36599707
Treatment of Ulcerative Colitis by Cationic Liposome Delivered NLRP3 siRNA [ Int J Nanomedicine, 2023, 18:4647-4662] PubMed: 37605735
Amiloride alleviates morphine tolerance by suppressing ASIC3-dependent neuroinflammation in the spinal cord [ Eur J Pharmacol, 2023, 10.1016/j.ejphar.2023.176173] PubMed: 37918499
Versatile Nano-PROTAC-Induced Epigenetic Reader Degradation for Efficient Lung Cancer Therapy [ Adv Sci (Weinh), 2022, 9(29):e2202039] PubMed: 35988145
Bile acids promote the caveolae-associated entry of swine acute diarrhea syndrome coronavirus in porcine intestinal enteroids [ PLoS Pathog, 2022, 18(6):e1010620] PubMed: 35696443

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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