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Submit ReviewSB 452533
Description: Potent TRPV1 antagonist
Chemical Name: N-(2-Bromophenyl)-N'-[2-[ethyl(3-methylphenyl)amino]ethyl]-urea
Purity: ≥98% (HPLC)
Biological Activity for SB 452533
SB 452533 is a 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
Technical Data for SB 452533
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for SB 452533
References for SB 452533
References are publications that support the biological activity of the product.
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, SB 452533 supplier, SB452533, TRPV1, transient, receptor, potential, channels, antagonists, vanilloid, receptors, analgesic, analgaesic, TRPV, 3265, 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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