Biological Activity
Selective CaV3.1 channel blocker (IC50 values are 0.2 and 31.8 μM for hCaV3.1 and hCaV3.2 respectively). Also reversibly inhibits NaV1.8 and blocks KV2.1 channels.
Technical Data
| M. Wt | 3987.51 |
| Formula | C171H245N53O47S6 |
| Sequence |
ECRYWLGGCSAGQTCCKHLVCSRRHGWCVWDGTFS (Modifications: Disulfide bridge: 2-16, 9-21, 15-28) |
| Storage | Store at -20°C |
| CAS Number | 484598-35-8 |
| PubChem ID | 90488963 |
| InChI Key | TYAZSKURKBASCY-UHFFFAOYSA-N |
| Smiles | [H]N[C@@H](CCC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)CNC(=O)[C@H](CC4=CNC=N4)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CC=C(O)C=C4)NC(=O)[C@H](CCCNC(N)=N)NC1=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N3)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](CCCCN)NC2=O)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CO)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3987.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 5 mM | 0.05 mL | 0.25 mL | 0.5 mL |
| 10 mM | 0.03 mL | 0.13 mL | 0.25 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.05 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ohkubo et al (2010) Tarantula toxin ProTx-I differentiates between human T-type voltage-gated Ca2+ channels Cav3.1 and Cav3.2. J.Pharmacol.Sci. 112 452 PMID: 20351484
Ohkubo and Yamazaki (2012) T-type voltage-activated calcium channel Cav3.1, but not Cav3.2, is involved in the inhibition of proliferation and apoptosis in MCF-7 human breast cancer cells. Int.J.Oncol. 41 267 PMID: 22469755
Middleton et al (2002) Two tarantula peptides inhibit activation of multiple sodium channels. Biochemistry 41 14734 PMID: 12475222
Keywords: ProTx I, supplier, ProTxI, calcium, sodium, potassium, ion, channels, NaV1.8, CaV3.1, CaV3.2, KV2.1, selective, blockers, venoms, Voltage-gated, Calcium, Channels, Voltage-gated, Sodium, Channels, Voltage-Gated, Potassium, Channels, Voltage-gated, Calcium, Channels, Tocris Bioscience
