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

GAL-021 

Cat. No.: HY-101422 Purity: 98.11%
Handling Instructions

GAL-021 a new intravenous BKCa-channel blocker.

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
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GAL-021 a new intravenous BKCa-channel blocker.

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].

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 morphine 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].

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

Molecular Weight

254.33

Formula

C₁₁H₂₂N₆O

CAS No.
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 : ≥ 30 mg/mL (117.96 mM)

*"≥" 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
10 mM 0.3932 mL 1.9659 mL 3.9319 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: 98.11%

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GAL-021
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