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GAL-021

GAL-021 an intravenous BKCa-channel blocker.

Catalog No. T3557Cas No. 1380341-99-0

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Purity:99.73%

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COA HPLC LCMS HNMR

GAL-021

Catalog No. T3557Cas No. 1380341-99-0

GAL-021 an intravenous BKCa-channel blocker.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
1 mg	$31	In Stock
5 mg	$68	In Stock
10 mg	$105	In Stock
25 mg	$197	In Stock
50 mg	$297	In Stock
100 mg	$459	In Stock
500 mg	$987	In Stock
1 mL x 10 mM (in DMSO)	$77	In Stock

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Product Introduction

Bioactivity

Description	GAL-021 an intravenous BKCa-channel blocker.
In vitro	Using inside-out patches in GH3 cells, GAL-021 concentration-dependently inhibits 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: 5 μM), and A3 (93% I; IC50: 1 μM) receptors, at 5-HT2B receptors (60% I; IC50: 30 μM).
In vivo	GAL-021 administered intravenously (i.v.) mitigates opiate-induced respiratory depression in both rats and nonhuman primates, preserving morphine's analgesic effects in rats. Furthermore, its capacity to stimulate ventilation in rats is diminished following carotid sinus nerve transection. This ventilatory stimulation by GAL-021 is also reduced in mice devoid of the pore-forming α-subunit of the KCa 1.1 channel.
Kinase Assay	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].
Alias	GAL 021

Chemical Properties

Molecular Weight	254.33
Formula	C₁₁H₂₂N₆O
Cas No.	1380341-99-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (196.59 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.9319 mL	19.6595 mL	39.3190 mL	196.5950 mL
5 mM	0.7864 mL	3.9319 mL	7.8638 mL	39.3190 mL
10 mM	0.3932 mL	1.9659 mL	3.9319 mL	19.6595 mL
20 mM	0.1966 mL	0.9830 mL	1.9659 mL	9.8297 mL
50 mM	0.0786 mL	0.3932 mL	0.7864 mL	3.9319 mL
100 mM	0.0393 mL	0.1966 mL	0.3932 mL	1.9659 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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