Biological Activity
Potent, selective and competitive vanilloid TRPV1 receptor antagonist (pA2 = 7.71 at hVR1); antagonizes hTRPV1 receptors activated by agonists, noxious heat, but not protons. Displays selectivity over a wide range of receptors and systems including CB1 and CB2 receptors, voltage-gated Ca2+ channels and the hyperpolarization-activated current (Ih). Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
SB 366791 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 287.75 |
| Formula | C16H14ClNO2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 472981-92-3 |
| PubChem ID | 667594 |
| InChI Key | RYAMDQKWNKKFHD-JXMROGBWSA-N |
| Smiles | COC1=CC=CC(NC(=O)C=CC2=CC=C(Cl)C=C2)=C1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.77 | 100 | |
| ethanol | 2.88 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 287.75. 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 | 3.48 mL | 17.38 mL | 34.75 mL |
| 5 mM | 0.7 mL | 3.48 mL | 6.95 mL |
| 10 mM | 0.35 mL | 1.74 mL | 3.48 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Fowler et al (2003) Inhibition of C6 glioma cell proliferation by anandamide, 1-arachidonylglycerol, and by a water soluble phosphate ester of anandamide: variability in response and involvement of arachidonic acid. Biochem.Pharmacol. 66 757 PMID: 12948856
Gavva et al (2005) Proton activation does not alter antagonist interaction with the capsaicin-binding pocket of TRPV1. Mol.Pharmacol. 68 1524 PMID: 16135784
Gunthorpe et al (2004) Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology 46 133 PMID: 14654105
Keywords: SB 366791, supplier, Potent, selective, competitive, TRPV1, VR1, antagonists, Vanillioids, Receptors, TRPV, Channels, Transient, Receptor, Potential, SB366791, GlaxoSmithKline, GSK, TRPV, TRPV, Tocris Bioscience
