484598-36-9
Chemical Structure
ProTx II
- CAS No.: 484598-36-9
- Formula:C168H250N46O41S8
- Molecular Weight:3826.59
SMILES: O=C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCC(O)=O)C(NCC(N[C@@H](CCSC)C(N[C@H]1C(C)C)=O)=O)=O)=O)NC2=O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCCN)C(N[C@@H](CC3=CNC4=CC=CC=C34)C(N[C@@H](CCSC)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H]([C@H](O)C)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@H]7CC8=CNC9=CC=CC=C89)=O)=O)=O)NC1=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CO)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@H]2CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CC%10=CNC%11=CC=CC=C%10%11)C(O)=O)=O)=O)=O)=O)=O)NC7=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC%12=CC=C(C=C%12)O)N
Biological Activity: ProTx II is a selective blocker of Nav1.7 sodium channels, with an IC50 value of 0.3 nM and a Ki of 0.389 nM against human NaV1.7. ProTx II selectively blocks spinal cord NaV1.7 by reducing conductance and altering voltage dependence of activation, preferentially binds to the splice region of aNaV1.5, and can also block sodium channel subtypes such as Nav1.4 and Nav1.6. ProTx II alleviates thermal hyperalgesia in diabetic mice and prevents the propagation of action potentials in nociceptors. ProTx II can be used for research related to painful diabetic neuropathy and pain disorders[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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ProTx II | 98.34% | ProTx II is a selective blocker of Nav1.7 sodium channels, with an IC50 value of 0.3 nM and a Ki of 0.389 nM against human NaV1.7. ProTx II selectively blocks spinal cord NaV1.7 by reducing conductance and altering voltage dependence of activation, preferentially binds to the splice region of aNaV1.5, and can also block sodium channel subtypes such as Nav1.4 and Nav1.6. ProTx II alleviates thermal hyperalgesia in diabetic mice and prevents the propagation of action potentials in nociceptors. ProTx II can be used for research related to painful diabetic neuropathy and pain disorders. | ||||||||||||||||||||
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References
- [1]. Tanaka K, et al. Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. Journal of experimental pharmacology. 2015;7:11-6. [Content Brief]
- [2]. Fraser SP, et al. Neonatal Na 1.5 channels: pharmacological distinctiveness of a cancer-related voltage-gated sodium channel splice variant. British journal of pharmacology. 2022 Feb;179(3):473-486.
- [3]. Schmalhofer WA, et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Molecular pharmacology. 2008 Nov;74(5):1476-84. [Content Brief]
