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Description: TRPC1 and TRPC6 blocker; inhibits mechanosensitive ion channels
Biological Activity
TRPC1 and TRPC6 blocker. Also blocks stretch-activated cation channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells. Also inhibits TACAN, a mechanosensitive ion channel involved in the pain response.
Licensing Information
Sold under license from The Research Foundation of The State University of New York
Technical Data
| M. Wt | 4095.86 |
| Formula | C185H273N49O45S6 |
| Sequence |
GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF (Modifications: Disulfide bridge: 2-17,9-23,16-30) (Modifications: Phe-34 = C-terminal amide) |
| Storage | Store at -20°C |
| PubChem ID | 90488987 |
| InChI Key | WVDNTWXIIKNMHY-UHFFFAOYSA-N |
| Smiles | [H]NCC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC1=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC2=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets
References
References are publications that support the biological activity of the product.
Bowman et al (2007) Mechanosensitive ion channels and the peptide inhibitor GsMTx-4: history, properties, mechanisms and pharmacology. Toxicon. 49 249 PMID: 17157345
Suchyna et al (2000) Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J.Gen.Physiol. 115 583 PMID: 10779316
Drew et al (2007) High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain. PLoS One 2 e515 PMID: 17565368
Bae et al (2011) The mechanosensitive ion channel Piezo1 is inhibited by the peptide GsMTx4. Biochemistry 50 6295 PMID: 21696149
Beaulieu-Laroche et al (2020) TACAN is an ion channel involved in sensing mechanical pain. Cell 180 956 PMID: 32084332
If you know of a relevant reference for GsMTx4, please let us know.
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Keywords: GsMTx4, GsMTx4 supplier, TRPC, transient, receptor, potential, TRPC1, and, TRPC6, mechanosensitive, ion, channels, MSCs, blockers, blocks, inhibits, inhibitors, venoms, TACAN, pain, TMEM120A, TMEM, Piezo, Channels, Other, Channel, Modulators, 4912, Tocris Bioscience
5 Citations for GsMTx4
Citations are publications that use Tocris products. Selected citations for GsMTx4 include:
Beaulieu-Laroche et al (2020) TACAN is an ion channel involved in sensing mechanical pain. Cell 180 956 PMID: 32084332
Dela Paz (2018) Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun 497 220 PMID: 29428723
Sun et al (2019) The mechanosensitive Piezo1 channel is required for bone formation. Elife 8 PMID: 31290742
Agbani et al (2018) Aquaporin-1 regulates platelet procoagulant membrane dynamics and in vivo thrombosis. JCI Insight 3 PMID: 29769447
Wong et al (2018) Mechanical Stretching Simulates Cardiac Physiology and Pathology through Mechanosensor Piezo1. J Clin Med 7 PMID: 30400259
Do you know of a great paper that uses GsMTx4 from Tocris? Please let us know.
Reviews for GsMTx4
Average Rating: 4 (Based on 1 Review.)
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Filter by:
a mechanosensitive channel blocker.
By
Hyun Choi on 02/19/2018
Assay Type: Ex Vivo
Species: Rat
Cell Line/Tissue: Applied to brain slices
It blocks mechanosensitive channels such as TRPC1 and 6.Dissolved in artificial cerebrospinal fluid (acsf) at 20 microM.
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