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Galicaftor

Cat. No. M29021
Galicaftor Structure
Synonym:

ABBV-2222; GLPG-2222

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Biological Activity

Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research.

Chemical Information
Molecular Weight 559.46
Formula C28H21F4NO7
CAS Number 1918143-53-9
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
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] Anna Lester, et al. Biochemistry. Computational Exploration of Potential CFTR Binding Sites for Type I Corrector Drugs

[2] Eric A Voight, et al. ACS Med Chem Lett. Fueling the Pipeline via Innovations in Organic Synthesis

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  Catalog
Abmole Inhibitor Catalog




Keywords: Galicaftor, ABBV-2222; GLPG-2222 supplier, CFTR, inhibitors, activators


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