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GAL-021

Cat. No. M14253
GAL-021 Structure
Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 210  USD210 In stock
50mg USD 630  USD630 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 254.33
CAS Number 1380341-99-0
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Te-Ling Lu, et al. High Efficacy by GAL-021: A Known Intravenous Peripheral Chemoreceptor Modulator that Suppresses BK Ca-Channel Activity and Inhibits IK(M) or Ih

[2] Marijke Hyke Algera, et al. Opioid-induced respiratory depression in humans: a review of pharmacokinetic-pharmacodynamic modelling of reversal

[3] Francis J Golder, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator

[4] Mark L Dallas, et al. GAL-021 and GAL-160 are Efficacious in Rat Models of Obstructive and Central Sleep Apnea and Inhibit BKCa in Isolated Rat Carotid Body Glomus Cells

[5] J F McLeod, et al. GAL-021, a new intravenous BKCa-channel blocker, is well tolerated and stimulates ventilation in healthy volunteers

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