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VX-150

Cat. No. M20814
VX-150 Structure
Synonym:

EOS-62073

Size Price Availability Quantity
5mg USD 300  USD300 In stock
10mg USD 460  USD460 In stock
25mg USD 900  USD900 In stock
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Quality Control & Documentation
Biological Activity

VX-150 (EOS-62073) is an orally bioavailable pro-drug that rapidly converts into its active moiety, which is a highly selective inhibitor of NaV1.8 relative to the other sodium channel subtypes (>400-fold).

Chemical Information
Molecular Weight 516.34
Formula C21H17F4N2O7P
CAS Number 1793080-72-4
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] Sascha R A Alles, et al. Front Pain Res (Lausanne). Peripheral Voltage-Gated Cation Channels in Neuropathic Pain and Their Potential as Therapeutic Targets

[2] Hemme J Hijma, et al. Pain Med. A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Pharmacodynamic Effects of VX-150, a Highly Selective NaV1.8 Inhibitor, in Healthy Male Adults

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  Catalog
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Keywords: VX-150, EOS-62073 supplier, Sodium Channel, inhibitors, activators


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