A BKCa channel blocker; inhibits BKCa single-channel activity in GH3 cells in a concentration-dependent manner from 1-10 μM; increases respiratory product minute volume in wild-type rats and mice (ED50s = 0.1 and 0.5 mg/kg); reverses morphine-induced respiratory depression in rats and cynomolgus monkeys; potentiates morphine-induced analgesia in a tail flick assay in rats

GAL-021 – 25 mg

Brand:
Cayman
CAS:
1380341-99-0
Storage:
-20
UN-No:
Non-Hazardous - /

GAL-021 is a large-conductance Ca2+-activated potassium channel (BKCa/KCa1.1) blocker.{45082} It inhibits BKCa single-channel activity in GH3 cells in a concentration-dependent manner when used at concentrations ranging from 1 to 10 μM. GAL-021 increases respiratory product minute volume in wild-type rats and mice (ED50s = 0.1 and 0.5 mg/kg) but not mice with bilaterally transected carotid sinus nerves or Slo-/- mice that lack the pore-forming α-subunit of BKCa. It reverses morphine-induced respiratory depression in rats and cynomolgus monkeys. GAL-021 also potentiates morphine-induced analgesia in a tail-flick assay in rats.  

 

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Description

A BKCa channel blocker; inhibits BKCa single-channel activity in GH3 cells in a concentration-dependent manner from 1-10 μM; increases respiratory product minute volume in wild-type rats and mice (ED50s = 0.1 and 0.5 mg/kg); reverses morphine-induced respiratory depression in rats and cynomolgus monkeys; potentiates morphine-induced analgesia in a tail flick assay in rats

Formal name: N2-methoxy-N2-methyl-N4,N6-dipropyl-1,3,5-triazine-2,4,6-triamine

Synonyms: 

Molecular weight: 254.3

CAS: 1380341-99-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Pain Research

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