SB 452533
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
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Keywords: SB452533 TRPV1 transient receptor potential channels antagonists vanilloid receptors analgesic analgaesic TRPV
1 Citation for SB 452533
Citations are publications that use Tocris products. Selected citations for SB 452533 include:
Vijayvergiya et al (2015) Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. Mol Pain 10 e0141366 PMID: 26513481
Do you know of a great paper that uses SB 452533 from Tocris? If so please let us know.
Literature in this Area
Pain Research Product Guide
A collection of over 250 products for pain research, the guide includes research tools for the study of:
- Nociception
- Ion Channels
- G-Protein-Coupled Receptors
- Intracellular Signaling
Pain Poster
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
