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SB-705498 | TRPV1 blocker

CAS:
501951-42-4
Catalog Number:
10-3985
Activity:
TRPV1 blocker
Chemical Names:
1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridine-2-yl]pyrrolidine-3-yl]urea
Molecular Weight:
429.24
Molecular Formula:
C17H16BrF3N4O
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

SB-705498 (501951-42-4) is a potent and selective blcoker of the TRPV1 receptor (IC50’s for receptor induction method: Capsaicin = 3 nM; Acid (pH5.3) = pIC50 7.1, and Heat = 6 nM) with activity in human, rat, and guinea pig receptors.1,2 SB-705498s activity is voltage dependent and shows >100 fold selectivity over the closely related TRPM8 receptor.2

References:

  1. Rami et al. (2006),  Discovery of SB-705498: a potent and orally bioavailable TRPV1 antagonist suitable for clinical development; Bioorg. Med. Chem. Lett., 16 3287
  2. Gunthorpe et al. (2007), 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., 321 1183
SB-705498 | TRPV1 blocker is also available in the Cellular Metabolism Library.
CAS:
501951-42-4
Catalog Number:
10-3985
Activity:
TRPV1 blocker
Chemical Names:
1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridine-2-yl]pyrrolidine-3-yl]urea
Molecular Weight:
429.24
Molecular Formula:
C17H16BrF3N4O
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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