2. Membrane Transporter/Ion Channel Anti-infection Apoptosis
  3. Sodium Channel HIV Apoptosis
  4. 5-(N,N-Hexamethylene)-amiloride

5-(N,N-Hexamethylene)-amiloride  (Synonyms: Hexamethylene amiloride; HMA)

Cat. No.: HY-128067 Purity: 98.47%
COA Handling Instructions

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5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.

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5-(N,N-Hexamethylene)-amiloride Chemical Structure

5-(N,N-Hexamethylene)-amiloride Chemical Structure

CAS No. : 1428-95-1

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

5-(N,N-Hexamethylene)-amiloride Related Antibodies

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2 Publications Citing Use of MCE 5-(N,N-Hexamethylene)-amiloride

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Description

5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively[1][2].

IC50 & Target

HIV-1

 

In Vitro

5-(N,N-Hexamethylene)-amiloride inhibits human cardiac ion channels hERG (in CHO cells), Nav1.5 and Cav1.2 (in EHK293 cells) with of 3.3 μM, 30 μM, 8.3 μM, respectively, inelectrophysiology assays[3].
5-(N,N-Hexamethylene)-amiloride (1 μM; 0-60 min; 37 ℃) exhibits microsomal stability, (1 μg/mL; 4.2 h; 37 ℃) shows mouse plasma stability and plasma protein binding, (20 μM; 4 h) displays Caco-2 cell permeability, cardiac ion channel activity[3].

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

5-(N,N-Hexamethylene)-amiloride Related Antibodies

Cell Viability Assay[3]

Cell Line: In vitro pharmacokinetics properties
Concentration: 1 μM
Incubation Time: 0-60 min
Result:
t1/2 (min) CLint (μL/min/mg protein) CLint (μL/min/mg protein)
Human liver microsomers in vitro 73 24 74
Mouse liver microsomers in vitro 2.4 726 2243
In Vivo

5-(N,N-Hexamethylene)-amiloride (2.5 mg/kg; i.v.; single dose) shows short half-life and lowly oral bioavailability of 4.5%[3].
In vivo pharmacokinetics in mice or rat model[3]
Dosage: 2.5 mg/kg Administration: Intravenous injection; single does; collected 10 min and 60 min after treatment.

t1/2 (h) Plasma CLint (mL/min/kg) Plasma Vss (L/kg) Plasma AUC0-inf (h·μM) B/P ratio Blood CL (mL/min/kg) Blood Vss (L/kg)
Female Balb/c mice 0.62 86 2.0 1.5 1.5 59 1.4
Sprague Dawley rats 3.2 83.5 5.3 1.6 1.8 46.2 2.9
% IV dose excreted in urine (0-24 h) Renal Blood CL (mL/min/kg) Non-Renal Blood CL (mL/min/kg)
Sprague Dawley rats 0.5 0.2 46.0
Note: B/P means blood-to-plasma partitioning ratio; female Balb/c mice (17-27 g, non-fasted); male Sprague Dawley rats (238-325 g, overnight-fasted).

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

311.77

Formula

C12H18ClN7O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=NC(Cl)=C(N2CCCCCC2)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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (320.75 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 3.2075 mL 16.0375 mL 32.0749 mL
5 mM 0.6415 mL 3.2075 mL 6.4150 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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: 2.08 mg/mL (6.67 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.08 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

Purity: 98.47%

COA (248 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2075 mL 16.0375 mL 32.0749 mL 80.1873 mL
5 mM 0.6415 mL 3.2075 mL 6.4150 mL 16.0375 mL
10 mM 0.3207 mL 1.6037 mL 3.2075 mL 8.0187 mL
15 mM 0.2138 mL 1.0692 mL 2.1383 mL 5.3458 mL
20 mM 0.1604 mL 0.8019 mL 1.6037 mL 4.0094 mL
25 mM 0.1283 mL 0.6415 mL 1.2830 mL 3.2075 mL
30 mM 0.1069 mL 0.5346 mL 1.0692 mL 2.6729 mL
40 mM 0.0802 mL 0.4009 mL 0.8019 mL 2.0047 mL
50 mM 0.0641 mL 0.3207 mL 0.6415 mL 1.6037 mL
60 mM 0.0535 mL 0.2673 mL 0.5346 mL 1.3365 mL
80 mM 0.0401 mL 0.2005 mL 0.4009 mL 1.0023 mL
100 mM 0.0321 mL 0.1604 mL 0.3207 mL 0.8019 mL
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5-(N,N-Hexamethylene)-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:

5-(N,N-Hexamethylene)-amiloride1428-95-1Hexamethylene amiloride HMASodium ChannelHIVApoptosisNa channelsNa+ channelsHuman immunodeficiency virusleukemic cellsHCoV229EMHVmouse hepatitis virusVpu virus ion channelInhibitorinhibitorinhibit

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