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Amiloride HCl (Synonyms: MK-870)

Catalog No.GC17853

L'amiloride HCl (chlorhydrate de MK-870) est un inhibiteur À la fois du canal sodique épithélial (ENaC[1]) et du récepteur de l'activateur du plasminogène de type urokinase (uTPA[2]).

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Amiloride HCl Chemical Structure

Cas No.: 2016-88-8

Taille Prix Stock Qté
10mM (in 1mL DMSO)
45,00 $US
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100mg
31,00 $US
En stock
500mg
66,00 $US
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

The epithelial sodium channel (ENaC) is a membrane-bound ion-channel that is permeable to protons, Li+-ions, and especially Na+-ions. It is a constitutively active ion-channel. It can be argued that it is the most selective ion channel. In vertebrates, the channels control reabsorption of sodium in kidney, colon, lung and sweat glands. They also play a role in taste perception. Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC).

In vitro: Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 of 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride completely inhibits Na+ influx in doses of 1.5 μM in vascular smooth muscle cells [1].

In vivo: Amiloride at 1 mg/kg/day is found to reverse the initial increases in collagen deposition and prevent further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the stroke-prone spontaneously hypertensive rats. Amiloride antagonizes or prevents actions of aldosterone in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension [1].

Clinical trial: Amiloride is a potassium-sparing diuretic, first approved for use in 1967, used in the management of hypertension and congestive heart failure. Amiloride was also tested as treatment of cystic fibrosis, but it was revealed inefficient in vivo due to its short time of action.

Reference:
[1] Teiwes J, Toto RD.  Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17.

Chemical Properties

Cas No. 2016-88-8 SDF
Synonymes MK-870
Chemical Name 3,5-diamino-6-chloro-N-(diaminomethylidene)pyrazine-2-carboxamide;hydrochloride
Canonical SMILES C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl
Formula C6H8ClN7O.HCl M.Wt 266.09
Solubility ≥ 13.3mg/mL in DMSO,6mg/ml in water。 Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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