Galicaftor (ABBV-2222)

Catalog No.S8535 Batch:S853501

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Technical Data

Formula

C28H21F4NO7
Molecular Weight 559.46 CAS No. 1918143-53-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (178.74 mM)
Ethanol 100 mg/mL (178.74 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
5% DMSO 95% Corn oil
2.5mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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%.

Protocol (from reference)

Cell Assay:

[2]
  • 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.

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

Primary human nasal epithelial cells: biobanking in the context of precision medicine [ Biology, 2022, (182)-] PubMed: None
Primary Human Nasal Epithelial Cells: Biobanking in the Context of Precision Medicine [ J Vis Exp, 2022, (182)] PubMed: 35532277

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.