SB 452533

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Cat.No. 3265 - SB 452533 | C18H22BrN3O | CAS No. 459429-39-1
Description: Potent TRPV1 receptor antagonist
Chemical Name: N-(2-Bromophenyl)-N'-[2-[ethyl(3-methylphenyl)amino]ethyl]-urea
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

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: SB 452533, supplier, SB452533, TRPV1, transient, receptor, potential, channels, antagonists, vanilloid, receptors, analgesic, analgaesic, TRPV, TRPV, Tocris Bioscience

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


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Literature in this Area

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
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  • G-Protein-Coupled Receptors
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Pain

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.

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