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Olacaftor

Cat. No. M29003
Olacaftor Structure
Synonym:

VX-440

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Biological Activity

Olacaftor (VX-440) is a cystic fibrosis transmembrane conductance regulator (CFTR) modulator extracted from patent US9782408.

Chemical Information
Molecular Weight 539.66
Formula C29H34FN3O4S
CAS Number 1897384-89-2
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic and warming and heat to 60°C)
Storage Powder -20°C
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] David P Nichols, et al. Am J Respir Crit Care Med. Clinical Effectiveness of Elexacaftor/Tezacaftor/Ivacaftor in People with Cystic Fibrosis: A Clinical Trial

[2] No authors listed. Med Lett Drugs Ther. Elexacaftor/tezacaftor/ivacaftor (Trikafta) for cystic fibrosis

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

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

[5] 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

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Keywords: Olacaftor, VX-440 supplier, CFTR, inhibitors, activators


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