Biological Activity
Potent and selective, voltage-dependent R-type CaV2.3 calcium channel blocker (IC50 = 30 nM). Antinociceptive; inhibits nociceptive C-fibre and Aδ-fibre-evoked neuronal responses.
Technical Data
M. Wt | 4495.01 |
Formula | C192H274N52O60S7 |
Sequence |
GVDKAGCRYMFGGCSVNDDCCPRLGCHSLFSYCAWDLTFSD (Modifications: Disulfide bridge between 7 - 21, 14 - 26, 20 - 33) |
Storage | Desiccate at -20°C |
CAS Number | 203460-30-4 |
PubChem ID | 90488787 |
InChI Key | NSUPRLHDCFNOKD-UHFFFAOYSA-N |
Smiles | [H]NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CC=C(O)C=C4)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC4=CNC=N4)NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CCSC)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)C)C(=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)N3)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]1CCCN1C2=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=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)N[C@@H](CC(O)=O)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 in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 4495.01. 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 | 0.22 mL | 1.11 mL | 2.22 mL |
5 mM | 0.04 mL | 0.22 mL | 0.44 mL |
10 mM | 0.02 mL | 0.11 mL | 0.22 mL |
50 mM | 0 mL | 0.02 mL | 0.04 mL |
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References
References are publications that support the products' biological activity.
Newcomb et al (1998) Selective peptide antagonist of the class E calcium channel from the venom of the Tarantula Hysterocrates gigas. Biochemistry 37 15353 PMID: 9799496
Bourinet et al (2001) Interaction of SNX482 with domains III and IV inhibits activation gating of α1E (CaV2.3) calcium channels. Biophys.J. 81 79 PMID: 11423396
Matthews et al (2007) The CaV2.3 calcium channel antagonist SNX-482 reduces dorsal horn neuronal responses in a rat model of chronic neuropathic pain. Eur.J.Neurosci. 25 3561 PMID: 17610575
Keywords: SNX 482, supplier, Potent, selective, CaV23, blockers, R-type, Calcium, CaV, Channels, R-Type, voltage-gated, voltage-dependent, Ca2+, SNX482, venoms, Voltage-gated, Calcium, Channels, Voltage-gated, Calcium, Channels, Tocris Bioscience