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

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.

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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
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10 mM * 1 mL in DMSO USD 72 In-stock
Solid
100 mg USD 66 In-stock
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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Amiloride:

Amiloride Related Antibodies

Top Publications Citing Use of Products

32 Publications Citing Use of MCE Amiloride

WB

    Amiloride purchased from MedChemExpress. 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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    TRPC TRPM TRPV TRPA TRPML

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]
    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against human HEK293 cells measured after 48 hrs by MTS assay
    Cytotoxicity against human HEK293 cells measured after 48 hrs by MTS assay
    		[PMID: 31679971]
    HEK293 IC50
    57 μM
    Compound: amiloride
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    		[PMID: 18788725]
    HepG2 IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against human HepG2 cells measured after 48 hrs by MTS assay
    Cytotoxicity against human HepG2 cells measured after 48 hrs by MTS assay
    		[PMID: 31679971]
    HT-1080 IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against human HT1080 cells measured after 48 hrs by MTS assay
    Cytotoxicity against human HT1080 cells measured after 48 hrs by MTS assay
    		[PMID: 31679971]
    MDA-MB-231 IC50
    > 100 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells measured after 48 hrs by MTS assay
    Cytotoxicity against human MDA-MB-231 cells measured after 48 hrs by MTS assay
    		[PMID: 31679971]
    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].

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

    Amiloride Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    229.63

    Formula

    C6H8ClN7O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N
    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 (435.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.3548 mL 21.7741 mL 43.5481 mL
    5 mM 0.8710 mL 4.3548 mL 8.7096 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (10.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (10.89 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.3548 mL 21.7741 mL 43.5481 mL 108.8703 mL
    5 mM 0.8710 mL 4.3548 mL 8.7096 mL 21.7741 mL
    10 mM 0.4355 mL 2.1774 mL 4.3548 mL 10.8870 mL
    15 mM 0.2903 mL 1.4516 mL 2.9032 mL 7.2580 mL
    20 mM 0.2177 mL 1.0887 mL 2.1774 mL 5.4435 mL
    25 mM 0.1742 mL 0.8710 mL 1.7419 mL 4.3548 mL
    30 mM 0.1452 mL 0.7258 mL 1.4516 mL 3.6290 mL
    40 mM 0.1089 mL 0.5444 mL 1.0887 mL 2.7218 mL
    50 mM 0.0871 mL 0.4355 mL 0.8710 mL 2.1774 mL
    60 mM 0.0726 mL 0.3629 mL 0.7258 mL 1.8145 mL
    80 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.3609 mL
    100 mM 0.0435 mL 0.2177 mL 0.4355 mL 1.0887 mL
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    Amiloride Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Amiloride2609-46-3MK-870MK870MK 870Sodium ChannelTRP ChannelApoptosisNa channelsNa+ channelsTransient receptor potential channelsInhibitorinhibitorinhibit

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