GpTx-1 TFA is a peptide-based Na V 1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na V 1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for Na V 1.4 ( IC50 = 0.301 μM) and Na V 1.5 ( IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively [1].
References:
[1]. Murray JK, et al. Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel. J Med Chem. 2015 Mar 12;58(5):2299-314.
References:
[1]. Murray JK, et al. Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel. J Med Chem. 2015 Mar 12;58(5):2299-314.