GNE-131
GNE-131 is a Potent and Selective hNaV1.7 Inhibitor (Na V1.7 IC50 = 3 nM) for the Treatment of Pain. 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.
For research use only. We do not sell to patients.
Chemical Information
| Name | GNE-131 |
|---|---|
| Iupac 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 |
| Molecular Formula | C23H30N4O3S |
| Molecular Weight | 442.58 |
| Smile | O=S(C1CC1)(NC2=NN=C3C=C(OCC45CC6CC(C5)CC(C6)C4)C(C7CC7)=CN32)=O |
| InChiKey | FPERPEQIXLOVIK-UHFFFAOYSA-N |
| InChi | 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) |
| CAS Number | 1629063-81-5 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. 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 May 8. doi: 10.1021/acs.jmedchem.7b01826. [Epub ahead of print] PubMed PMID: 29737846.
Chemical Structure
