1. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis
  2. Sodium Channel TRP Channel Apoptosis
  3. Amiloride

Amiloride  (Synonyms: MK-870)

Cat. No.: HY-B0285
Handling Instructions

Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Amiloride hydrochloride dihydrate and Amiloride hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Amiloride Chemical Structure

Amiloride Chemical Structure

CAS No. : 2609-46-3

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Top Publications Citing Use of Products

    Amiloride purchased from MCE. Usage Cited in: Microb Pathog. 2019 Jul 18:103638.   [Abstract]

    The viral mRNA and VP1 protein levels in IBRS-2 cells treated with different concentrations of Amiloride are determined by qPCR and Western Blot, respectively. ‘‘VC’’ indicates that the cells that are not treated with Amiloride.

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    Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC[1]) and urokinase-type plasminogen activator receptor (uTPA[2]). Amiloride is a blocker of polycystin-2 (PC2; TRPP2[3]) channel.

    IC50 & Target

    ENaC[1]; uTPA[2]; polycystin-2(TRPP2)[3]

    In Vitro

    Amiloride blocks δβγ channels with an IC50 of 2.6 μM (58, 71, 75, 134, 148). The Ki of amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The Ki of amiloride for δαβγ channels is 920 and 13.7 μM at -120 and +80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels[1]. 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)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Amiloride (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[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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    Room temperature in continental US; may vary elsewhere.


    Please store the product under the recommended conditions in the Certificate of Analysis.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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