GpTx-1 TFA 

GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively^[1].

4073.82 (free base)

C₁₇₆H₂₇₁N₅₃O₄₅S₇.xC₂HF₃O₂

Solid

White to off-white

Asp-Cys-Leu-Gly-Phe-Met-Arg-Lys-Cys-Ile-Pro-Asp-Asn-Asp-Lys-Cys-Cys-Arg-Pro-Asn-Leu-Val-Cys-Ser-Arg-Thr-His-Lys-Trp-Cys-Lys-Tyr-Val-Phe-NH2 (Disulfide bridge: Cys2-Cys17;Cys9-Cys23;Cys16-Cys30)

DCLGFMRKCIPDNDKCCRPNLVCSRTHKWCKYVF-NH2 (Disulfide bridge: Cys2-Cys17;Cys9-Cys23;Cys16-Cys30)

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]

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]