Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
GNE-131 is a novel, potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM. The sodium channel NaV1.7 has emerged as a promising target for the treatment of pain based on strong genetic validation of its role in nociception. In recent years, a number of aryl and acyl sulfonamides have been reported as potent inhibitors of NaV1.7, with high selectivity over the cardiac isoform NaV1.5. GNE-131 showed excellent potency, good in vitro metabolic stability, and low in vivo clearance in mouse, rat, and dog. GNE-131 also displayed excellent efficacy in a transgenic mouse model of induced pain.
ln Vitro |
GNE-131 (Compound 13) had a 0.003±0.001 μM IC50 against human NaV1.7 and moderate clearance in human liver microsomes. It also demonstrated high functional activity against the virus. In vitro metabolic stability and potency of GNE-131 are both good [1].
|
---|---|
ln Vivo |
In vivo clearance of GNE-131 is poor in rats, mice, and dogs. Excellent efficacy of GNE-131 has also been demonstrated in transgenic mouse models of pain [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
|
Molecular Formula |
C23H30N4O3S
|
---|---|
Molecular Weight |
442.574304103851
|
CAS # |
1629063-81-5
|
SMILES |
O=S(C1CC1)(NC2=NN=C3C=C(OCC45CC6CC(C5)CC(C6)C4)C(C7CC7)=CN32)=O
|
InChi Key |
FPERPEQIXLOVIK-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C23H30N4O3S/c28-31(29,18-3-4-18)26-22-25-24-21-8-20(19(12-27(21)22)17-1-2-17)30-13-23-9-14-5-15(10-23)7-16(6-14)11-23/h8,12,14-18H,1-7,9-11,13H2,(H,25,26)
|
Chemical Name |
N-(7-(Adamantan-1-ylmethoxy)-6-cyclopropyl-[1,2,4]-triazolo[4,3-a]-pyridin-3-yl)cyclo-propanesulfonamide
|
Synonyms |
GNE-131; GNE 131; GNE131
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~125 mg/mL (~282.44 mM)
|
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2595 mL | 11.2976 mL | 22.5953 mL | |
5 mM | 0.4519 mL | 2.2595 mL | 4.5191 mL | |
10 mM | 0.2260 mL | 1.1298 mL | 2.2595 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.