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VX-661

Cat. No. M3128
VX-661 Structure
Synonym:

Tezacaftor

Size Price Availability Quantity
5mg USD 90  USD90 In stock
25mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Vx-661 is the second F508del CFTR correction compound that assists the CFTR protein to reach the cell surface.

Chemical Information
Molecular Weight 520.5
Formula C26H27F3N2O6
CAS Number 1152311-62-0
Solubility (25°C) DMSO 90 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] Ana M Matos, et al. Treatment of Polarized Cystic Fibrosis Airway Cells With HGF Prevents VX-661-Rescued F508del-CFTR Destabilization Caused by Prolonged Co-exposure to VX-770

[2] Gabriella Fűr, et al. Mislocalization of CFTR expression in acute pancreatitis and the beneficial effect of VX-661 + VX-770 treatment on disease severity

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

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

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

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  Catalog
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Keywords: VX-661, Tezacaftor supplier, CFTR, inhibitors, activators


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