484598-35-8
Chemical Structure
ProTx-I
- CAS No.: 484598-35-8
- Formula:C171H245N53O47S6
- Molecular Weight:3987.49
SMILES: O=C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CC1=CNC=N1)C(N[C@@H](CC(C)C)C(N[C@H]2C(C)C)=O)=O)=O)=O)NC3=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC4=CC=C(C=C4)O)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H](CC(C)C)C(NCC(NCC(N[C@@H](CSSC[C@@H](C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC7=CNC=N7)C(NCC(N[C@H]8CC9=CNC%10=CC=CC=C9%10)=O)=O)=O)=O)=O)=O)NC2=O)C(N[C@@H](CO)C(N[C@@H](C)C(NCC(N[C@@H](CCC(N)=O)C(N[C@@H]([C@H](O)C)C(N[C@H]3CSSC[C@@H](C(N[C@@H](C(C)C)C(N[C@@H](CC%11=CNC%12=CC=CC=C%11%12)C(N[C@@H](CC(O)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC%13=CC=CC=C%13)C(N[C@@H](CO)C(O)=O)=O)=O)=O)=O)=O)=O)=O)NC8=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCC(O)=O)N
Biological Activity:
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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ProTx-I | 95.15% | ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC50 values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba2+ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain. |
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- [1]. Rupasinghe DB, et al. Mutational analysis of ProTx-I and the novel venom peptide Pe1b provide insight into residues responsible for selective inhibition of the analgesic drug target NaV1.7. Biochem Pharmacol. 2020;181:114080. [Content Brief]
- [2]. Ohkubo T, et al. Tarantula toxin ProTx-I differentiates between human T-type voltage-gated Ca2+ Channels Cav3.1 and Cav3.2. J Pharmacol Sci. 2010;112(4):452-458. [Content Brief]
- [3]. Priest BT, et al. ProTx-I and ProTx-II: gating modifiers of voltage-gated sodium channels. Toxicon. 2007;49(2):194-201. [Content Brief]
Keywords
