GNE-131|cas 1629063-81-5|DC Chemicals

Cas No.:	1629063-81-5
Chemical Name:	GNE-131
Synonyms:	GNE-131;gne-131;GNE131;GNE 131;CS-2887;Cyclopropanesulfonamide, N-[6-cyclopropyl-7-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-1,2,4-triazolo[4,3-a]pyridin-3-yl]-;N-[6-Cyclopropyl-7-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-1,2,4-triazolo[4,3-a]pyridin-3-yl]cyclopropanesulfonamide
SMILES:	C1(S(NC2N3C(=NN=2)C=C(OCC24CC5CC(CC(C5)C2)C4)C(C2CC2)=C3)(=O)=O)CC1
Formula:	C₂₃H₃₀N₄O₃S
M.Wt:	442.574304103851
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
Target:	IC50: 3 nM (hNaV1.7)[1].
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[1].
In Vitro:	GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability[1].
References:	[1]. Focken T, et al. 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. J Med Chem. 2018 Jun 14;61(11):4810-4831.

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