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SB-705498

A Blocker of TRPV1 Channels

Cat #: S-160
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 428.05
    Purity: >99%
    Form Lyophilized powder.
    Effective concentration 10 nM - 50 µM.
    Structure
    Chemical name (R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)ureaN-(2-bromophenyl)-N?-[((R)-1-(5-trifluoromethyl-2-pyridyl)pyrrolidin-3-yl)]urea.
    Molecular formula C17H16BrF3N4O.
    CAS No.: 501951-42-4
    Activity SB-705498 is a potent orally active TRPV1 blocker1.
    References-Activity
    1. Gunthorpe, M.J. et al. (2007) J. Pharmacol. Exp. Ther. 321, 1183.
    2. Kort, M.E. and Kym, P.R. (2012) Prog. Med. Chem. 51, 57.
    3. Szallasi, A. et al. (2007) Nat. Rev. Drug Discov. 6, 357.
    4. Conway, S.J. (2008) Chem. Soc. Rev. 37, 1530.
    5. Holland, C. et al. (2014) Br. J. Clin. Pharmacol. 77, 777.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO 100 mM. Centrifuge all product preparations before use (10000 x g 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs SB-705498 inhibits TRPV1 channels heterologously expressed in C-6 cells.
      Alomone Labs SB-705498 inhibits TRPV1 channels heterologously expressed in C-6 cells.
      Cells were loaded with Fluo-3 AM and changes in intracellular Ca2+ were detected. Normalized fluorescence of control cells (untreated and unstimulated), cells responding to 1µM Capsaicin (#C-125), with or without pre-incubation with 10 µM SB-705498 (#S-160), as indicated.
    References - Scientific background
    1. Kort, M.E. and Kym, P.R. (2012) Prog. Med. Chem. 51, 57.
    2. Szallasi, A. et al. (2007) Nat. Rev. Drug Discov. 6, 357.
    3. Conway, S.J. (2008) Chem. Soc. Rev. 37, 1530.
    4. Holland, C. et al. (2014) Br. J. Clin. Pharmacol. 77, 777.
    Scientific background

    SB-705498 is a specific and potent antagonist for TRPV1. Generally, TRPV1 inhibitors are classified as either both capsaicin and proton blockers, and mainly capsaicin blockers. SB-705498 belongs to the first class2. After experimenting with lesser potent and effective antagonists, the major advantageous modification the compound's developers had introduced into the related TRPV1 archetypal inhibitors was a trifluoromethyl-substituted pyridine ring; it presented SB-705498 with good solubility and oral bioavailability, superior pharmacokinetic properties1-3.

    SB-705498 was developed as an intranasal medication for the treatment of neuropathic and inflammatory pain. Recent clinical trials checked the effectiveness of the compound in treating rhinitis, alleviating dental pain, and relieving acute migraine headache2,4.

    Target TRPV1 channels
    Last update: 11/04/2021

    SB-705498 (#S-160) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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