Home Transmembrane Transporters CFTR modulator Galicaftor (ABBV-2222)

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Galicaftor (ABBV-2222) CFTR modulator

Cat.No.S8535

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

Chemical Structure

Molecular Weight: 559.46

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (178.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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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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Chemical Information, Storage & Stability

Molecular Weight 559.46 Formula

C28H21F4NO7

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1918143-53-9 -- Storage of Stock Solutions

Synonyms GLPG2222 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

Mechanism of Action

Targets/IC50/Ki
CFTR
In vitro

Galicaftor (ABBV-2222) exhibits potent in vitro functional activity in primary patient cells harboring F508del/F508del CFTR with an EC50 <10 nM. It promotes maturation of F508delCFTR, stabilizes nucleotide binding domain 1 - membrane spanning domain interface, and corrects F508delCFTR through action on membrane spanning domain 1.
In vivo

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

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