GLPG-2222( ABBV-2222 | ABBV2222 | GLPG2222 )

Catalog No. M13006 CAS No. 1918143-53-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GLPG-2222
Note

Research use only, not for human use.
Brief Description

GLPG-2222 (ABBV-2222, Galicaftor) is a novel potent and efficacious CFTR corrector with EC50 of 5 nM; is highly potent (5 nM) and efficacious in cells from multiple CF patient donors that have F508del homozygous mutation.
Description

GLPG-2222 (ABBV-2222, Galicaftor) is a novel potent and efficacious CFTR corrector with EC50 of 5 nM; is highly potent (5 nM) and efficacious in cells from multiple CF patient donors that have F508del homozygous mutation; shows potential in clinical trials in patients harboring the F508del CFTR mutation on at least one allele.Cystic Fibrosis,Phase 2 Clinical.
In Vitro

Galicaftor (ABBV-2222; GLPG-2222) exhibits potent in vitro functional activity in primary patient cells harboring F508del/F508del CFTR, with an EC50 <10 nM.
In Vivo

The rat pharmacokinetic tests are performed on Galicaftor (ABBV-2222; GLPG-2222; 1 mg/kg, i.v.; 1 mg/kg, p.o.) to illustrate its pharmacokinetic properties in rats. The T1/2 is 2.7 hours (i.v.). And for intragastric administration, the bioavailability (%F) is 74%.
Synonyms

ABBV-2222 | ABBV2222 | GLPG2222
Pathway

Apoptosis
Target

CFTR
Recptor

CFTR
Research Area

Other Indications
Indication

Fibrosis

CAS Number

1918143-53-9
Formula Weight

559.47
Molecular Formula

C28H21F4NO7
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 50 mg/mL (89.37 mM)
SMILES

FC(F)OC1=CC=C2C(O[C@@H](C3=CC=C(C(O)=O)C=C3)C[C@H]2NC(C4(C5=CC(OC(F)(F)O6)=C6C=C5)CC4)=O)=C1
Chemical Name

4-[(2R,4R)-4-({[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic acid

1. Wang X, et al. J Med Chem. 2017 Dec 18. doi: 10.1021/acs.jmedchem.7b01339.

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