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Elexacaftor (VX-445)

Cat. No. M10162
Elexacaftor (VX-445) Structure
Synonym:

VX-445

Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

Elexacaftor (VX-445) is a next-generation modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445) has the potential to treat cystic fibrosis. VX-445-Tezacaftor-VX-770 significantly improves Phe508del CFTR protein processing, trafficking, and chloride transport to a greater extent than any two of these agents in dual combination.

Chemical Information
Molecular Weight 597.65
Formula C26H34F3N7O4S
CAS Number 2216712-66-0
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] Peter G Middleton, et al. N Engl J Med. Elexacaftor-Tezacaftor-Ivacaftor for Cystic Fibrosis with a Single Phe508del Allele

[2] Dominic Keating, et al. N Engl J Med. VX-445-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles

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