A TRPV1 antagonist
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SB-705498

Item No. 17313

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]-urea
CAS Number
501951-42-4
Molecular Formula
C17H16BrF3N4O
Formula Weight
429.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 16 mg/mlEthanol: 10 mg/ml
λmax
257, 312 nm
SMILES
BrC1=C(NC(N[C@@H]2CCN(C3=NC=C(C(F)(F)F)C=C3)C2)=O)C=CC=C1
InChi Code
InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-5-11(9-22-15)17(19,20)21/h1-6,9,12H,7-8,10H2,(H2,23,24,26)/t12-/m1/s1
InChi Key
JYILLRHXRVTRSH-GFCCVEGCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $43

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    5 mg

    $76

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    10 mg

    $129

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    Product Description

    SB-705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated activation of TRPV1 receptors (pKis = 7.6, 7.5, and 7.3 for human, rat, and guinea pig, respectively).1 It has been shown to induce rapid, reversible inhibition of capsaicin (IC50 = 3 nM)-, acid (pH 5.3)-, or heat (50°C; IC50 = 6 nM)-mediated activation of human TRPV1 (at -70 mV).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gunthorpe, M.J., Hannan, S.L., Smart, D., 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. 321(3), 1183-1192 (2007).