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GNE-131

Cat. No. M9129
GNE-131 Structure
Synonym:

GNE131

Size Price Availability Quantity
10mM*1mL USD 490  USD490 In stock
2mg USD 330  USD330 In stock
5mg USD 440  USD440 In stock
10mg USD 645  USD645 In stock
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Quality Control & Documentation
Biological Activity

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM. GNE-131 shows excellent potency, good in vitro metabolic stability. 

In vivo, GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain.

Chemical Information
Molecular Weight 442.57
Formula C23H30N4O3S
CAS Number 1629063-81-5
Solubility (25°C) DMSO: ≥ 90 mg/mL (Need ultrasonic)
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] Focken T, et al. J Med Chem. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.

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  Catalog
Abmole Inhibitor Catalog




Keywords: GNE-131, GNE131 supplier, Sodium Channel, inhibitors, activators


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