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

Amiloride (hydrochloride)  (Synonyms: アミロリド塩酸塩; MK-870 hydrochloride)

製品番号: HY-B0285A 純度: 99.84%
COA 取扱説明書 Technical Support

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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CAS 番号 : 2016-88-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 在庫あり
Solution
10 mM * 1 mL in DMSO USD 72 在庫あり
Solid
100 mg $66 在庫あり
500 mg $119 在庫あり
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カスタマーレビュー

Based on 62 publication(s) in Google Scholar

Other Forms of Amiloride hydrochloride:

Amiloride (hydrochloride) 関連抗体

Top Publications Citing Use of Products

顧客検証

IF
Cell Imaging/Staining
WB
Flow Cytometry
RT-PCR

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2025 Aug 3.

    Typical confocal images of RAW 264.7 cells incubated with 100 µg/mL FITC/M-BSA@PSiNPs for 6 h, in the absence or presence of Amiloride（50 μM; 6 h).

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2025 Aug 3.

    The inhibitory effects of Pitstop 2, MβCD, Amiloride (50 μM; 6 h) and CytoD on the expression of IL-1β, IL-6, CCL2, IFN-β, CXCL10 and TNF-α genes in RAW 264.7 cells.

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2025 Aug 3.

    Typical confocal images of RAW 264.7 cells incubated with 100 μg/mL FITC/M-BSA@PSiNPs for 6 h, in the absence or presence of 50 μmol/L Pitstop 2, 100 μmol/L Methyl-β-cyclodextrin (MβCD), 50 μmol/L amiloride, or 1 μmol/L CytoD (scale bar = 40 μm).

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2024 Dec;14(12):5418-5434.

    Amiloride hydrochloride (450 μM; 4 h) profoundly impaired the uptake rates of Il2/ZIF-8@Salmonella in RAW264.7 cells.

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(9):e2307880.  [Abstract]

    Representative images and quantitative data of the NIR fluorescent signals in H9C2 cells exposed to IR‐780 pre‐treatment with ice condition, Amiloride (75 µg/mL; 30 min).

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Bone marrow cells cultured in medium containing 10 ng/mL GM-CSF for 3 days were treated with 2 μg PKH67-labeled sEVs with or without Amiloride (10 μM), Chlorpromazine (10 μM), or EIPA (5 μM) for 1 h. The median fluorescence intensity (MFI) of PKH67 was assessed by flow cytometry.

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Amiloride hydrochloride (10 μM; 3 d) crippled the effect of shNT cell-derived sEVs in elevating MDSCs to the level of shXBP cell-generated sEVs.

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Amiloride hydrochloride (10 μM; 3 d) decreased the STAT3 phosphorylation level in MDSCs.

    Amiloride hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):2018-2035.e8.  [Abstract]

    Amiloride hydrochloride (10 μM; 3 d) decreased the iNOS mRNA level in MDSCs.

    Amiloride hydrochloride 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.

    Sodium Channel アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

    TRP Channel アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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    製品説明

    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]
    体外実験

    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].

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

    Amiloride (hydrochloride) 関連抗体
    体内実験

    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.
    臨床実験
    分子量

    266.09

    分子式

    C6H9Cl2N7O
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N.Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (375.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

    V2

    体内:

    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 (9.40 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 (9.40 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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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.
    純度とドキュメンテーション

    純度: 99.84%

    COA (248 KB) HNMR (271 KB) RP-HPLC (243 KB) MS (68 KB)

    取扱説明書 (2659 KB)
    参考文献

    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 3.7581 mL 18.7906 mL 37.5813 mL 93.9532 mL
    5 mM 0.7516 mL 3.7581 mL 7.5163 mL 18.7906 mL
    10 mM 0.3758 mL 1.8791 mL 3.7581 mL 9.3953 mL
    15 mM 0.2505 mL 1.2527 mL 2.5054 mL 6.2635 mL
    20 mM 0.1879 mL 0.9395 mL 1.8791 mL 4.6977 mL
    25 mM 0.1503 mL 0.7516 mL 1.5033 mL 3.7581 mL
    DMSO 30 mM 0.1253 mL 0.6264 mL 1.2527 mL 3.1318 mL
    40 mM 0.0940 mL 0.4698 mL 0.9395 mL 2.3488 mL
    50 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8791 mL
    60 mM 0.0626 mL 0.3132 mL 0.6264 mL 1.5659 mL
    80 mM 0.0470 mL 0.2349 mL 0.4698 mL 1.1744 mL
    100 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Amiloride hydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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      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:

    Amiloride2016-88-8MK-870MK870MK 870Sodium ChannelTRP ChannelApoptosisNa channelsNa+ channelsTransient receptor potential channelsInhibitorinhibitorinhibit

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    製品名:
    Amiloride hydrochloride
    製品番号:
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