Bioactivity | ProTx-III is a selective and potent inhibitor of voltage-gated sodium channel Nav1.7, with an IC50 of 2.1 nM. ProTx-III is a spider venom peptide isolated from the venom of the Peruvian green velvet tarantella. ProTx-III has a typical inhibitor cystine knot motif (ICK). ProTx-III is able to reverse the pain response. ProTx-III can be used to study diseases such as chronic pain, epilepsy, and arrhythmia[1]. |
Invitro | 原生,重组和合成的 C-末端酸和酰胺形式的 ProTx-III抑制 hNaV1.7 的 IC50 值分别为 2.1, 9.5, 11.5 和 2.5 nM[1]。ProTx-III 抑制 hNav1.7,而不显著改变激活或失活的电压依赖性[1]。 |
In Vivo | ProTx-III (0.01-1 μM; 足底注射) 在小鼠模型中可逆转通过足底内注射 OD1 诱导的小鼠自发性疼痛,从而证明其具有镇痛作用[1]。 Animal Model: |
Name | ProTx-III |
Sequence | Asp-Cys-Leu-Lys-Phe-Gly-Trp-Lys-Cys-Asn-Pro-Arg-Asn-Asp-Lys-Cys-Cys-Ser-Gly-Leu-Lys-Cys-Gly-Ser-Asn-His-Asn-Trp-Cys-Lys-Leu-His-Ile-NH2 (Disulfide bonds: Cys2-Cys17, Cys9-Cys22, Cys16-Cys29) |
Shortening | DCLKFGWKCNPRNDKCCSGLKCGSNHNWCKLHI (Disulfide bonds: Cys2-Cys17, Cys9-Cys22, Cys16-Cys29) |
Formula | C162H246N52O43S6 |
Molar Mass | 3802.40 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Cardoso FC, et al. Identification and Characterization of ProTx-III [μ-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens. Mol Pharmacol. 2015 Aug;88(2):291-303. |