Size | Price | Stock | Qty |
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100mg |
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250mg |
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500mg |
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1g |
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25g |
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Other Sizes |
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Purity: ≥98%
Amiloride HCl dihydrate (MK870; MK-870; MK 870; Midamor; Midoride; Modamide), the hydrochloride salt and dihydrated form of amiloride, is a potent and selective epithelial sodium channel (ENaC) blocker that has been used since 1967 in the management of hypertension and congestive heart failure.
Targets |
ENaC; uTPA; polycystin-2 (TRPP2)
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ln Vitro |
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ln Vivo |
A strong inhibitor of epithelial sodium channels (ENaCs) is amiloride hydrochloride dihydrate. Within fifteen to thirty minutes after injection, amiloride is significantly concentrated in the plasma. When compared to the baseline readings (n = 7), a 2 mg/kg dose of amiloride hydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, or hindquarters vascular resistance. Amiloride hydrochloride dihydrate causes very little change in heart rate (-10±6 bpm/min) and arterial pressure (-1±1 mmHg) over a 2-hour period when compared to baseline values. The c-Fos activation in the area postrema (AP) exhibits a dose-related response pattern, according to the results. Amiloride hydrochloride dihydrate, even at the lowest dose of 0.1 mg/kg, is statistically different from the control rats in terms of the number of c-Fos labeled neurons at the p<0.01 level[1].
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Cell Assay |
This study examined the mechanism of action of amiloride, a urokinase-type plasminogen activator receptor inhibitor, in lowering proteinuria. Podocytes were resuscitated to allow for their proliferation and were observed for morphological changes. In the in vitro experiment, control, lipopolysaccharide, and lipopolysaccharide + amiloride groups were established. The expression of urokinase-type plasminogen activator receptor (uPAR) in podocytes was detected with a flow cytometer and cell motility was detected with the transwell migration assay[2].
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Animal Protocol |
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References |
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Additional Infomation |
Amiloride hydrochloride dihydrate is a hydrate that is the dihydrate of amiloride hydrochloride. It has a role as a diuretic and a sodium channel blocker. It contains an amiloride hydrochloride.
Amiloride Hydrochloride is the hydrochloride salt of amiloride, a synthetic pyrazine derivative with antikaliuretic and diuretic properties. Amiloride inhibits sodium channels located in the distal tubules and collecting ducts of the kidney, thereby preventing the absorption of sodium and increasing its excretion along with water, to produce naturesis. In response to the hypernatremic conditions in the kidney, the plasma membrane becomes hyperpolarized and electrochemical forces are reduced, which then prevents the excretion of potassium and hydrogen into the lumen. A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705) |
Molecular Formula |
C6H8CLN7O.HCL.2H2O
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Molecular Weight |
302.12
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Exact Mass |
301.045
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Elemental Analysis |
C, 23.85; H, 4.34; Cl, 23.47; N, 32.45; O, 15.89
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CAS # |
17440-83-4
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Related CAS # |
Amiloride hydrochloride;2016-88-8;Amiloride;2609-46-3
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PubChem CID |
68540
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Appearance |
Typically exists as Off-white to yellow solids at room temperature
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Boiling Point |
628.1ºC at 760 mmHg
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Melting Point |
>240℃
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Flash Point |
333.7ºC
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Vapour Pressure |
1.08E-15mmHg at 25°C
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LogP |
1.944
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Hydrogen Bond Donor Count |
7
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Hydrogen Bond Acceptor Count |
7
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Rotatable Bond Count |
1
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Heavy Atom Count |
18
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Complexity |
279
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Defined Atom Stereocenter Count |
0
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SMILES |
ClC1C(N([H])[H])=NC(=C(C(/N=C(\N([H])[H])/N([H])[H])=O)N=1)N([H])[H].Cl[H].O([H])[H].O([H])[H]
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InChi Key |
LTKVFMLMEYCWMK-UHFFFAOYSA-N
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InChi Code |
1S/C6H8ClN7O.ClH.2H2O/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;2*1H2
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Chemical Name |
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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: ≥ 2.5 mg/mL (8.27 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 (8.27 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: ≥ 2.08 mg/mL (6.88 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 | 3.3099 mL | 16.5497 mL | 33.0994 mL | |
5 mM | 0.6620 mL | 3.3099 mL | 6.6199 mL | |
10 mM | 0.3310 mL | 1.6550 mL | 3.3099 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.