| Identification | Back Directory | [Name]
ProTx II | [CAS]
484598-36-9 | [Synonyms]
PT-II
ProTx II
ProToxin-II
ProTx II USP/EP/BP | [Molecular Formula]
C168H250N46O41S8 | [MDL Number]
MFCD16876402 | [MOL File]
484598-36-9.mol | [Molecular Weight]
3826.59 |
| Questions And Answer | Back Directory | [Uses]
ProTx-II is a potent, selective Nav1.7 blocker. Voltage-gated sodium channels (Nav) are responsible for transducing extracellular signals into action potentials in excitable cells. The Nav1 family consists of nine sub-types for which selective tools are highly valued. Discovery of subtype-selective tools has been challenging due to conservation of putative binding sites. Nav1.7 is expressed in sensory neurons and is critical for pain processing. ProTx-II, isolated from the tarantula Thrixopelma pruriens, is a potent blocker of Nav1 channels. Although ProTx-II blocks several members of this channel family, it has >100-fold selectivity for Nav1.7. ProTx-II is active in an in vitro model of pain processing. ProTx-II binds to a previously unknown site on the channel, conferring selectivity and increasing its value as a research tool. It blocks Nav1.7 by decreasing conductance and shifting the activation potential in the positive direction, resulting in an overall decrease in excitability. |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
Soluble to 0.10 mg/ml in 4:1 Acetonitrile : water | [form ]
Powder | [color ]
White to off-white | [Water Solubility ]
Soluble to 1 mg/ml in water | [Sequence]
Tyr-Cys-Gln-Lys-Trp-Met-Trp-Thr-Cys-Asp-Ser-Glu-Arg-Lys-Cys-Cys-Glu-Gly-Met-Val-Cys-Arg-Leu-Trp-Cys-Lys-Lys-Lys-Leu-Trp (Disulfide bridge:Cys2-Cys16;Cys9-Cys21;Cys15-Cys25) |
| Hazard Information | Back Directory | [IC 50]
Nav1.7 | [storage]
Store at -20°C | [References]
[1] Tanaka K, et al. Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. J Exp Pharmacol. 2015 Jun 24;7:11-6. DOI:10.2147/JEP.S79973
[2] Schmalhofer WA, et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol. 2008 Nov;74(5):1476-84. DOI:10.1124/mol.108.047670 |
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BOC Sciences
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https://www.bocsci.com |
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