SB 452533

Key Product Details

Product Description

SB 452533 is a potent TRPV1 antagonist against capsaicin (pK_b = 7.7), noxious heat and acid-mediated (pIC₅₀ = 7.0) receptor activation (pK_i = 6.22 at the recombinant hTRPV1 receptor). Exhibits analgesic properties.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Product Specifications for SB 452533

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for SB 452533

The following data is based on the product molecular weight 376.29.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Weil Conservation of functional and pharmacological properties in the distantly related temperature sensors TRPV1 and TRPM8. Mol.Pharmacol. 2005 PMID: 15911692
• Bianchi [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. 2007 PMID: 17660385
• Rami Discovery of small molecule antagonists of TRPV1. Bioorg.Med.Chem.Lett. 2004 PMID: 15203132

Product Documents for SB 452533