Description
GAL-021 a new intravenous BKCa-channel blocker.
Product information
CAS Number: 1380341-99-0
Molecular Weight: 254.33
Formula: C11H22N6O
Chemical Name: N2-methoxy-N2-methyl-N4,N6-dipropyl-1,3,5-triazine-2,4,6-triamine
Smiles: CON(C)C1N=C(NCCC)N=C(NCCC)N=1
InChiKey: FJNLCHNQVJVCPY-UHFFFAOYSA-N
InChi: InChI=1S/C11H22N6O/c1-5-7-12-9-14-10(13-8-6-2)16-11(15-9)17(3)18-4/h5-8H2,1-4H3,(H2,12,13,14,15,16)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 30 mg/mL (117.96 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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).
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.
Products are for research use only. Not for human use.
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