Among the inhibitors of Nav1.7, a 34-residue peptide cross-linked by three disulfide bridges, named GpTx-1 which was isolated from the venom of the tarantula spider Grammostola porteri, is a potential lead molecule for the development of a novel analgesic targeting NaV1.7. Its analogue GpTx-1-71 of [Ala5,Phe6,Leu26,Arg28]-GpTx-1 (Figure 1) which was screened from hundreds of analogues by Amgen, exhibited exceptional NaV1.7 IC50 value of 1.6 nM and >1000x selectivity against NaV1.4 and NaV1.5.
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