Cat. No. Name Size Price Add Cart
KI2003SB-7054985 mg$432
SB-70549810 mg$592
SB-70549850 mg$1712
SB-705498200 mg$3952

Chemical Characteristic

Product NameSB-705498
SynonymsN/A
CAS No.501951-42-4
Molecular Weight 429.23
FormulaC17H16BrF3N4O
Chemical Name(R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea
SmilesN(C(=O)NC1CN(CC1)c1ccc(cn1)C(F)(F)F)c1c(cccc1)Br
Chemical Structure

Biological activities

SB-705498 is a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist. SB-705498 strongly and competitively inhibits the capsaicin-mediated activation of the human TRPV1 receptor, rat TRPV1 receptor, and guinea pig TRPV1 receptor with pKi values of 7.6, 7.5, and 7.3, respectively. SB-705498 inhibits capsaicin, acid, and heat activation of TRPV1 with IC50s of 3, 0.1 and 6 nM, respectively.[1] In the capsaicin-induced secondary hyperalgesia model, SB-705498 also shows antagonist activity against the specific TRPV1 agonist capsaicin.[2]

References

[1] Gunthorpe MJ, et al. Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor. J Pharmacol Exp Ther. 2007, 321(3): 1183-1192.
[2] Rami HK, et al. Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett. 2006, 16(12): 3287-3291.

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