GpTx-1 (TFA)

GpTx-1 TFA is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the NaV1.7 channel with an IC50 value of 10 nM, while exhibiting excellent selectivity for NaV1.4 (IC50 = 0.301 μM) and NaV1.5 (IC50 = 4.20 μM), showing >20-fold and >950-fold selectivity respectively[1].

Product Specifications

UNSPSC

12352209

Target

Sodium Channel

Related Pathways

Membrane Transporter/Ion Channel

Field of Research

Neurological Disease

Purity

99.56

Smiles

O=C([C@@H](N)CC(O)=O)N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N1[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]2CSSC[C@H](NC3=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC4=CC=CC=C4)=O)C(C)C)=O)CC5=CC=C(O)C=C5)=O)CCCCN)=O)=O)CCCCN)=O)CC(O)=O)=O)CC(N)=O)=O)CC(O)=O)=O)CCC1)=O)[C@H](CC)C)=O)CSSCC(NC6=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]3CC7=CNC8=CC=CC=C78)=O)CCCCN)=O)CC9=CNC=N9)=O)[C@@H](C)O)=O)CCCNC(N)=N)=O)CO)=O)=O)CCCCN)=O)CCCNC(N)=N)=O)CCSC)=O)CC%10=CC=CC=C%10)=O)=O)CC(C)C)=O)CSSC[C@H](NC2=O)C(N[C@H](C(N%11[C@H](C(N[C@H](C(N[C@H](C(N[C@H]6C(C)C)=O)CC(C)C)=O)CC(N)=O)=O)CCC%11)=O)CCCNC(N)=N)=O.O=C(C(F)(F)F)O.[x]

Molecular Formula

C176H271N53O45S7.xC2HF3O2

Molecular Weight

4073.82 (free base)

References & Citations

[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.