ABBV-2222 (GLPG2222)
ABBV-2222 (GLPG2222) Basic information
- Product Name:
- ABBV-2222 (GLPG2222)
- Synonyms:
-
- ABBV-2222 (GLPG2222)
- ABBV2222
- ABBV-2222
- GLPG-2222 (ABBV-2222)
- Galicaftor (ABBV-2222)
- Galicaftor
- Benzoic acid, 4-[(2R,4R)-4-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-7-(difluoromethoxy)-3,4-dihydro-2H-1-benzopyran-2-yl]-
- Galicaftor/ABBV-2222/GLPG-2222/
- CAS:
- 1918143-53-9
- MF:
- C28H21F4NO7
- MW:
- 559.46
- Mol File:
- 1918143-53-9.mol
ABBV-2222 (GLPG2222) Chemical Properties
- Boiling point:
- 701.1±60.0 °C(Predicted)
- Density
- 1.56±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (89.37 mM; Need ultrasonic)
- pka
- 4.16±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- InChIKey
- QVDYQHXNAQHIKH-TZIWHRDSSA-N
- SMILES
- C(O)(=O)C1=CC=C([C@@H]2OC3=CC(OC(F)F)=CC=C3[C@H](NC(C3(C4=CC=C5OC(F)(F)OC5=C4)CC3)=O)C2)C=C1
ABBV-2222 (GLPG2222) Usage And Synthesis
Uses
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[1].
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%[1].
References
[1] Xueqing Wang, et al. Discovery of 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 (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator DOI:10.1021/acs.jmedchem.7b01339
[2] Ashvani K Singh, et al. Biological Characterization of F508delCFTR Protein Processing by the CFTR Corrector ABBV-2222/GLPG2222. J Pharmacol Exp Ther. 2020 Jan;372(1):107-118. DOI:10.1124/jpet.119.261800
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