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GLPG-3221

Names

[ CAS No. ]:
2222264-64-2

[ Name ]:
GLPG-3221

Biological Activity

[Description]:

GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> CFTR
Research Areas >> Others

[In Vivo]

GLPG-3221 (1 mg/kg; i.v.) treatment shows the Cl and t1/2 are 0.13 L/h/kg and 3 hours, respectively[1]. GLPG-3221 (1 mg/kg; p.o.)treatment shows the F% value is 53%[1]. Animal Model: Rat[1]  Dosage: 1 mg/kg Administration: i.v. administration (Pharmacokinetic Analysis) Result: The Cl and t1/2 were 0.13 L/h/kg and 3 hours, respectively.

[References]

[1]. Scanio MJC, et al.Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.ACS Med Chem Lett. 2019 Oct 31;10(11):1543-1548.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H37F3N2O6

[ Molecular Weight ]:
578.62

Related Compounds