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

Amiloride hydrochloride (Synonyms: MK-870 hydrochloride)

Cat. No.: HY-B0285A Purity: 99.71%
Handling Instructions

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

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Amiloride hydrochloride Chemical Structure

Amiloride hydrochloride Chemical Structure

CAS No. : 2016-88-8

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Amiloride hydrochloride:

Top Publications Citing Use of Products

    Amiloride hydrochloride purchased from MCE. Usage Cited in: Microb Pathog. 2019 Jul 18:103638. 

    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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    Description

    Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC[1]) and urokinase-type plasminogen activator receptor (uTPA[2]). Amiloride hydrochloride 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. 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].

    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].

    Clinical Trial
    Molecular Weight

    266.09

    Formula

    C₆H₉Cl₂N₇O

    CAS No.

    2016-88-8

    SMILES

    O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (375.81 mM)

    H2O : 7.14 mg/mL (26.83 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    AmilorideMK-870MK870MK 870Sodium ChannelTRP ChannelApoptosisNa channelsNa+ channelsTransient receptor potential channelsInhibitorinhibitorinhibit

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    Amiloride hydrochloride
    Cat. No.:
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