Biological Activity
Potent TRPV1 antagonist against capsaicin (pKb = 7.7), noxious heat and acid-mediated (pIC50 = 7.0) receptor activation (pKi = 6.22 at the recombinant hTRPV1 receptor). Exhibits analgesic properties.
Licensing Information
Sold for research purposes only under agreement from GlaxoSmithKline
Compound Libraries
SB 452533 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 376.29 |
| Formula | C18H22BrN3O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 459429-39-1 |
| PubChem ID | 9842609 |
| InChI Key | IFJYEGJUQIBBQV-UHFFFAOYSA-N |
| Smiles | CC1=CC(N(CC)CCNC(NC2=CC=CC=C2Br)=O)=CC=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 | 37.63 | 100 | |
| ethanol | 3.76 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 376.29. 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 | 2.66 mL | 13.29 mL | 26.58 mL |
| 5 mM | 0.53 mL | 2.66 mL | 5.32 mL |
| 10 mM | 0.27 mL | 1.33 mL | 2.66 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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References
References are publications that support the products' biological activity.
Rami et al (2004) Discovery of small molecule antagonists of TRPV1. Bioorg.Med.Chem.Lett. 14 3631 PMID: 15203132
Weil et al (2005) Conservation of functional and pharmacological properties in the distantly related temperature sensors TRPV1 and TRPM8. Mol.Pharmacol. 68 518 PMID: 15911692
Bianchi et al (2007) [3H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-ylurea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J.Pharmacol.Exp.Ther. 323 285 PMID: 17660385
Keywords: SB 452533, supplier, SB452533, TRPV1, transient, receptor, potential, channels, antagonists, vanilloid, receptors, analgesic, analgaesic, TRPV, TRPV, Tocris Bioscience
