Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G610616-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $680.90 | |
G610616-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,360.90 |
Synonyms | compound 24;GNE616 |
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Specifications & Purity | Moligand™ |
Grade | Moligand™ |
Action Type | CHANNEL BLOCKER |
Mechanism of action | Channel blocker of Na v1.1;Channel blocker of Na v1.2;Channel blocker of Na v1.3;Channel blocker of Na v1.4;Channel blocker of Na v1.5;Channel blocker of Na v1.6;Channel blocker of Na v1.7 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (4S)-6-fluoro-4-[(2R,4S)-2-(pyridin-2-yl)-4-(trifluoromethyl)piperidin-1-yl]-N-(pyrimidin-4-yl)-3,4-dihydro-2H-1-benzopyran-7-sulfonamide |
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INCHI | InChI=1S/C24H23F4N5O3S/c25-17-12-16-19(33-9-5-15(24(26,27)28)11-20(33)18-3-1-2-7-30-18)6-10-36-21(16)13-22(17)37(34,35)32-23-4-8-29-14-31-23/h1-4,7-8,12-15,19-20H,5-6,9-11H2,(H,29,31,32)/t15-,19-,20+/m0/s1 |
InChi Key | XQUOWYVEKSXNET-RYGJVYDSSA-N |
Canonical SMILES | Fc1cc2c(cc1S(=O)(=O)Nc1ccncn1)OCC[C@@H]2N1CC[C@@H](C[C@@H]1c1ccccn1)C(F)(F)F |
Isomeric SMILES | C1CN([C@H](C[C@H]1C(F)(F)F)C2=CC=CC=N2)[C@H]3CCOC4=CC(=C(C=C34)F)S(=O)(=O)NC5=NC=NC=C5 |
PubChem CID | 138393286 |
PubChem CID | 138393286 |
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Enter Lot Number to search for COA:
1. Goldberg YP, MacFarlane J, MacDonald ML, Thompson J, Dube MP, Mattice M, Fraser R, Young C, Hossain S, Pape T, Payne B, Radomski C, Donaldson G, Ives E, Cox J, Younghusband HB, Green R, Duff A, Boltshauser E, Grinspan GA, Dimon JH, Sibley BG, Andria G, Toscano E, Kerdraon J, Bowsher D, Pimstone SN, Samuels ME, Sherrington R, Hayden MR. (2007) Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations.. Clin Genet, 71 (4): (311-9). [PMID:17470132] [10.1021/op500134e] |
2. Cox JJ, Reimann F, Nicholas AK, Thornton G, Roberts E, Springell K, Karbani G, Jafri H, Mannan J, Raashid Y et al.. (2006) An SCN9A channelopathy causes congenital inability to experience pain.. Nature, 444 (7121): (894-8). [PMID:17167479] [10.1021/op500134e] |
3. Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA. (2014) Recent progress in sodium channel modulators for pain.. Bioorg Med Chem Lett, 24 (16): (3690-9). [PMID:25060923] [10.1021/op500134e] |
4. Gingras J, Smith S, Matson DJ, Johnson D, Nye K, Couture L, Feric E, Yin R, Moyer BD, Peterson ML et al.. (2014) Global Nav1.7 knockout mice recapitulate the phenotype of human congenital indifference to pain.. PLoS ONE, 9 (9): (e105895). [PMID:25188265] [10.1021/op500134e] |
5. McKerrall SJ, Sutherlin DP. (2018) Nav1.7 inhibitors for the treatment of chronic pain.. Bioorg Med Chem Lett, 28 (19): (3141-3149). [PMID:30139550] [10.1021/op500134e] |
6. Shields SD, Deng L, Reese RM, Dourado M, Tao J, Foreman O, Chang JH, Hackos DH. (2018) Insensitivity to Pain upon Adult-Onset Deletion of Nav1.7 or Its Blockade with Selective Inhibitors.. J Neurosci, 38 (47): (10180-10201). [PMID:30301756] [10.1021/op500134e] |
7. McKerrall SJ, Nguyen T, Lai KW, Bergeron P, Deng L, DiPasquale A, Chang JH, Chen J, Chernov-Rogan T, Hackos DH et al.. (2019) Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.. J Med Chem, 62 (8): (4091-4109). [PMID:30943032] [10.1021/op500134e] |