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Icenticaftor

Cat. No. M21140
Icenticaftor Structure
Synonym:

QBW251

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Biological Activity

Icenticaftor (QBW251) is an oral enhancer of the cystic fibrosis transmembrane conductance regulator (CFTR) channel with an EC50 of 79 nM for F508del and 497 nM for G551D CFTR. Icenticaftor can be used in chronic obstructive pulmonary disease (COPD) and cystic fibrosis studies.

Chemical Information
Molecular Weight 361.24
Formula C12H13F6N3O3
CAS Number 1334546-77-8
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Laura Carrasco-Hernndez, et al. Biomedicines. Dysfunction in the Cystic Fibrosis Transmembrane Regulator in Chronic Obstructive Pulmonary Disease as a Potential Target for Personalised Medicine

[2] Darren Le Grand, et al. J Med Chem. Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease

[3] Shamsah Kazani, et al. J Cyst Fibros. Safety and efficacy of the cystic fibrosis transmembrane conductance regulator potentiator icenticaftor (QBW251)

[4] Steven M Rowe, et al. Int J Chron Obstruct Pulmon Dis. Efficacy and Safety of the CFTR Potentiator Icenticaftor (QBW251) in COPD: Results from a Phase 2 Randomized Trial

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