Home Transmembrane Transporters CFTR modulator Galicaftor (ABBV-2222) For research use only.

Galicaftor (ABBV-2222)

Synonyms: GLPG2222

Galicaftor (ABBV-2222, GLPG2222) is a potent corrector of CFTR for the treatment of Cystic Fibrosis (CF).

Galicaftor (ABBV-2222) Chemical Structure

Galicaftor (ABBV-2222) Chemical Structure

CAS: 1918143-53-9

Selleck's Galicaftor (ABBV-2222) has been cited by 2 publications

Purity & Quality Control

Batch: S853501 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 98.93%
98.93

Galicaftor (ABBV-2222) Related Products

Signaling Pathway

CFTR Signaling Pathways

CFTR Signaling Pathway

Choose Selective CFTR Inhibitors

Biological Activity

Description Galicaftor (ABBV-2222, GLPG2222) is a potent corrector of CFTR for the treatment of Cystic Fibrosis (CF).
Targets
CFTR [1]
In vitro
In vitro

ABBV-2222/GLPG2222 exhibits potent in vitro functional activity in primary patient cells harboring F508del/F508del CFTR with an EC50 <10 nM. ABBV-2222 promotes maturation of F508delCFTR, and stabilizes nucleotide binding domain 1 - membrane spanning domain interface. ABBV-2222 corrects F508delCFTR through action on membrane spanning domain 1.[2]
Cell Research Cell lines CFBE41o-F508del CFTR-HRP cells
Concentrations 0 - 20 μM
Incubation Time 18-24 h
Method

 ABBV-2222/GLPG2222 is then added at the required concentrations and further incubated for 18-24 hours at 33 °C. The highest concentration tested is 20 μM with an 8-12 point concentration response curve using a 3-fold dilution.
In Vivo
In vivo

Pharmacokinetic tests are performed in rats on Galicaftor (ABBV-2222; GLPG-2222; 1 mg/kg, i.v.; 1 mg/kg, p.o.) showed T1/2 is 2.7 hours (i.v.) and for intragastric administration, the bioavailability (%F) is 74%.

Chemical Information & Solubility

Molecular Weight 559.46 Formula

C28H21F4NO7
CAS No. 1918143-53-9 SDF --
Smiles C1CC1(C2=CC3=C(C=C2)OC(O3)(F)F)C(=O)NC4CC(OC5=C4C=CC(=C5)OC(F)F)C6=CC=C(C=C6)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (178.74 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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