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CFTR corrector 12

Cat. No. M42171
CFTR corrector 12 Structure
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Biological Activity

CFTR corrector 12 is a bithiazole derivative, serving as CFTR corrector.

Chemical Information
Molecular Weight 436.98
Formula C19H21ClN4O2S2
CAS Number 958941-60-1
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] Kaden Ridley et al. J Pediatr Pharmacol Ther. Elexacaftor-Tezacaftor-Ivacaftor: The First Triple-Combination Cystic Fibrosis Transmembrane Conductance Regulator Modulating Therapy

[2] Sheridan M Hoy. Drugs. Elexacaftor/Ivacaftor/Tezacaftor: First Approval

[3] Peter G Middleton et al. N Engl J Med. Elexacaftor-Tezacaftor-Ivacaftor for Cystic Fibrosis with a Single Phe508del Allele

[4] Harry G M Heijerman et al. Lancet. Efficacy and safety of the elexacaftor plus tezacaftor plus ivacaftor combination regimen in people with cystic fibrosis homozygous for the F508del mutation: a double-blind, randomised, phase 3 trial

[5] Elena Fernandez Fernandez et al. Expert Rev Respir Med. CFTR dysfunction in cystic fibrosis and chronic obstructive pulmonary disease

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