1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. GAL-021

GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates.

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

GAL-021 Chemical Structure

GAL-021 Chemical Structure

CAS No. : 1380341-99-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 145 In-stock
Solution
10 mM * 1 mL in DMSO USD 145 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 198 In-stock
50 mg USD 594 In-stock
100 mg USD 990 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of GAL-021:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates[1][2].

In Vitro

GAL-021 is being developed as a novel breathing control modulator to preserve respiratory drive and protect patients from respiratory impairment due to opioids and other modalities. Using inside-out patches in GH3 cells, GAL-021 exerts concentration-dependent inhibition of single-channel KCa1.1 activity. When evaluated against 12 different cardiac ion channels, inhibition is 35% or less at 30 μM. No significant kinase inhibition is observed at 10 μM. At 30 μM in the radioligand binding assays, interactions (defined as >50% radioligand displacement) are detected at adenosine A1 (65% I), A2A (79% I, IC50 approximately 5μM), and A3 (93% I; IC50 approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC50 approximately 30 μM)[1].

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

In Vivo

Intravenously administered GAL-021 attenuates opiate-induced respiratory depression in rats and nonhuman primates without affecting analgesia in rats. GAL-021 ventilatory stimulation in rats is attenuated by carotid sinus nerve transection. GAL-021 ventilatory stimulation is attenuated in mice lacking the pore-forming α-subunit of the KCa 1.1 channel[1].

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

Molecular Weight

254.33

Formula

C11H22N6O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCNC1=NC(N(OC)C)=NC(NCCC)=N1

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 : ≥ 30 mg/mL (117.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9319 mL 19.6595 mL 39.3190 mL
5 mM 0.7864 mL 3.9319 mL 7.8638 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.

  • 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: ≥ 2.08 mg/mL (8.18 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 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 (8.18 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: 99.89%

References
Kinase Assay
[1]

GAL-021 is dissolved in DMSO, and final assay concentration of DMSO is 0.1% or less. The effects of GAL-021 (30 μM) on a panel of 55 receptors, transporters, and ion channels are evaluated using radioligand binding analyses. Potential kinase inhibition by GAL-021 (10 μM) is assessed using the Kinase HotSpot Screen where activity of 50 kinases is measured in the presence of adenosine triphosphate (10 μM)[1].

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

Animal Administration
[1]

Rats: The effects of GAL-021 on mean arterial pressure (MAP) and heart rate (HR) are evaluated using IV infusions. GAL-021 (0.125 mg /kg/min for 25 min, increasing to 0.20 mg/kg/min for an additional 25 min IV) and vehicle (0.9% saline, for 50 min) are administered at a constant infusion rate (6 mL/kg/h). All rats receive additional fluid support (50:50 mixture of lactated Ringer's solution and 6% hetastarch in 0.9% saline at 4 mL/kg/min)[1]. For rat and Mouse Spirometry section, for rats, tracheal airflow is measured using flow spirometry before and after IV (femoral vein) bolus administration of GAL-021 (0.01, 0.03, 0.1, 0.3, 1.0, and 3.0 mg/kg) and vehicle (0.9% saline)[1].

Mice: The effects of GAL-021 on ventilation are also evaluated in age-matched male and female adult Slo1+/+ and Slo1-/- mice. Mice are anesthetized using 2 to 2.5% isoflurane in air[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, 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 3.9319 mL 19.6595 mL 39.3190 mL 98.2975 mL
5 mM 0.7864 mL 3.9319 mL 7.8638 mL 19.6595 mL
10 mM 0.3932 mL 1.9659 mL 3.9319 mL 9.8297 mL
15 mM 0.2621 mL 1.3106 mL 2.6213 mL 6.5532 mL
20 mM 0.1966 mL 0.9830 mL 1.9659 mL 4.9149 mL
25 mM 0.1573 mL 0.7864 mL 1.5728 mL 3.9319 mL
30 mM 0.1311 mL 0.6553 mL 1.3106 mL 3.2766 mL
40 mM 0.0983 mL 0.4915 mL 0.9830 mL 2.4574 mL
50 mM 0.0786 mL 0.3932 mL 0.7864 mL 1.9659 mL
60 mM 0.0655 mL 0.3277 mL 0.6553 mL 1.6383 mL
80 mM 0.0491 mL 0.2457 mL 0.4915 mL 1.2287 mL
100 mM 0.0393 mL 0.1966 mL 0.3932 mL 0.9830 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GAL-021 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GAL-021
Cat. No.:
HY-101422
Quantity:
MCE Japan Authorized Agent: