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

Amiloride hydrochloride dihydrate  (Synonyms: MK-870 hydrochloride dihydrate)

Cat. No.: HY-B0285B Purity: 99.85%
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Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel.

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

Amiloride hydrochloride dihydrate Chemical Structure

Amiloride hydrochloride dihydrate Chemical Structure

CAS No. : 17440-83-4

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10 mM * 1 mL in DMSO
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Based on 26 publication(s) in Google Scholar

Other Forms of Amiloride hydrochloride dihydrate:

Amiloride hydrochloride dihydrate Related Antibodies

Top Publications Citing Use of Products

    Amiloride hydrochloride dihydrate 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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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

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

    Amiloride hydrochloride dihydrate is a potent epithelial sodium channels (ENaCs) blocker. Amiloride is highly concentrated in the plasma 15 to 30 minutes following the injections. 2 mg/kg dose of Amiloride hydrochloride dihydrate has no effect on blood pressure, heart rate, mesenteric vascular resistance, or hindquarters vascular resistance as compare to the baseline measurements (n=7). Over a 2 hour period, Amiloride hydrochloride dihydrate elicits negligible responses in arterial pressure (-1±1 mmHg) and heart rate (-10±6 bpm/min) as compare to baseline levels. Results show an Amiloride hydrochloride dihydrate dose-related response pattern for the c-Fos activation in the area postrema (AP). Even at the lowest dose of Amiloride hydrochloride dihydrate (0.1 mg/kg), the number of c-Fos labeled neurons in the AP is statistically different from the control rats at a p<0.01 level[1].

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

    302.12

    Formula

    C6H13Cl2N7O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(C1=NC(Cl)=C(N)N=C1N)NC(N)=N.[H]Cl.O.O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 83.33 mg/mL (275.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 2 mg/mL (6.62 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3099 mL 16.5497 mL 33.0994 mL
    5 mM 0.6620 mL 3.3099 mL 6.6199 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)

    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 (8.27 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 (8.27 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.
    Purity & Documentation

    Purity: 99.85%

    COA (252 KB) HNMR (277 KB) RP-HPLC (260 KB) MS (70 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    The experiments are performed on male and female Sprague-Dawley rats that have been maintained in a heat controlled room maintained at 23° C with a 12h/12h light-dark schedule. A total of 116 adult rats are injected i.p. with Amiloride hydrochloride dihydrate (0.1, 0.5, and 2.0 mg/kg). After 15, 30, 45, or 120 min post-injection, the rats are anesthetized with 8% chloral hydrate, the chest is opened, and blood samples are obtained by cardiac puncture. The blood is centrifuged at 5000 RPM for 5 min, and the plasma (1.5 mL) separated and stored at -80° C[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 (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 3.3099 mL 16.5497 mL 33.0994 mL 82.7486 mL
    5 mM 0.6620 mL 3.3099 mL 6.6199 mL 16.5497 mL
    DMSO 10 mM 0.3310 mL 1.6550 mL 3.3099 mL 8.2749 mL
    15 mM 0.2207 mL 1.1033 mL 2.2066 mL 5.5166 mL
    20 mM 0.1655 mL 0.8275 mL 1.6550 mL 4.1374 mL
    25 mM 0.1324 mL 0.6620 mL 1.3240 mL 3.3099 mL
    30 mM 0.1103 mL 0.5517 mL 1.1033 mL 2.7583 mL
    40 mM 0.0827 mL 0.4137 mL 0.8275 mL 2.0687 mL
    50 mM 0.0662 mL 0.3310 mL 0.6620 mL 1.6550 mL
    60 mM 0.0552 mL 0.2758 mL 0.5517 mL 1.3791 mL
    80 mM 0.0414 mL 0.2069 mL 0.4137 mL 1.0344 mL
    100 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8275 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 dihydrate Related Classifications

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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.

    Keywords:

    Amiloride hydrochloride dihydrate17440-83-4MK-870 hydrochloride dihydrateSodium ChannelApoptosisTRP ChannelNa channelsNa+ channelsTransient receptor potential channelsInhibitorinhibitorinhibit

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