Funapide - CAS 1259933-16-8
Catalog number: 1259933-16-8
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Sodium Channel
Funapide is a Nav1.7 and Nav1.8 voltage-gated sodium channel inhibitor under the development by Xenon Pharmaceuticals and Teva Pharmaceutical Industries. It is applicated for the treatment of a variety of chronic painconditions, including osteoarthritis, neuropathic pain, postherpetic, neuralgia, erythromelalgia and dental pain. In July 2014, Funapide has reached phase IIb clinical trials.
UNII-A5595LHJ2L; A5595LHJ2L; XEN-401-S; TV-45070; (7S)-1'-[[5-(trifluoromethyl)furan-2-yl]methyl]spiro[6H-furo[2,3-f][1,3]benzodioxole-7,3'-indole]-2'-one
Soluble in DMSO
-20°C Freezer
chronic painconditions
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Teva Pharmaceutical Industries; Xenon Pharmaceuticals
1.Iron(III)-Catalyzed Arylation of Spiro-Epoxyoxindoles with Phenols/Naphthols towards the Synthesis of Spirocyclic Oxindoles.
Luo M;Yuan R;Liu X;Yu L;Wei W Chemistry. 2016 Jul 4;22(28):9797-803. doi: 10.1002/chem.201601185. Epub 2016 May 31.
An efficient and highly regioselective iron(III)-catalyzed Friedel-Crafts-type arylation of spiro-epoxyoxindoles with phenols was developed for rapid access to 3-(3-indolyl)-oxindole-3-methanols, which could be further elaborated into benzofuranyl-spirooxindoles under Mitsunobu conditions. When spiro-epoxyoxindoles were reacted with naphthols in the presence of a catalytic amount of FeCl3 ⋅6 H2 O in dichloromethane, they underwent a tandem Friedel-Crafts-type arylation and O-cyclization to yield novel naphthofuranyl-spirooxindoles in excellent yields. This method is applied to enable the efficient and highly regioselective synthesis of a small-molecule inhibitor of the sodium channel Nav 1.7 (±)-XEN402, which is currently in a phase IIb clinical trial for the treatment of pain.
2.Recent progress in sodium channel modulators for pain.
Bagal SK;Chapman ML;Marron BE;Prime R;Storer RI;Swain NA Bioorg Med Chem Lett. 2014 Aug 15;24(16):3690-9. doi: 10.1016/j.bmcl.2014.06.038. Epub 2014 Jun 21.
Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav drug discovery is an exciting field. Pharmaceutical investment in Navs for pain therapeutics has expanded exponentially due to genetic data such as SCN10A mutations and an improved ability to establish an effective screen sequence for example IonWorks Barracuda®, Synchropatch® and Qube®. Moreover, emerging clinical data (AZD-3161, XEN402, CNV1014802, PF-05089771, PF-04531083) combined with recent breakthroughs in Nav structural biology pave the way for a future of fruitful prospective Nav drug discovery.
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