| Chemical Properties | Back Directory | [Sequence]
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) |
| Hazard Information | Back Directory | [Uses]
GpTx-1 is a peptide-based NaV1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 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]. | [IC 50]
Nav1.3: 0.0203 μM (IC50); Nav1.4: 0.301 μM (IC50); Nav1.5: 4.20 μM (IC50); Nav1.7: 10 nM (IC50); Nav1.8: 12.2 μM (IC50) | [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. DOI:10.1021/jm501765v |
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| Company Name: |
Alomone Labs
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| Tel: |
4008-168-068 13121892008 |
| Website: |
www.alomone.com |
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