SB705498

For research use only.

Catalog No.S2773

2 publications

SB705498 Chemical Structure

Molecular Weight(MW): 429.23

SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2.

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Selleck's SB705498 has been cited by 2 publications

1 Customer Review

  • (B) SK-N-SH cells were incubated with AM251 (CB1 antagonist) or SB705498 (TRPV-1 antagonist) for 30 min and stimulated with NADA (10 μM) for 6 h. The expression of HIF-1α protein was determined by immunoblot analysis. We show a representative blot of three independent experiments.

    Biochim Biophys Acta, 2014, 1843:2730-2743.. SB705498 purchased from Selleck.

Purity & Quality Control

Choose Selective TRP Channel Inhibitors

Biological Activity

Description SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2.
Targets
hTRPV1 [1]
()
hTRPV1 [1]
()
7.6(pKi) 7.1(pIC50)
In vitro

SB705498 (0.3 nM-1 μM) potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. SB705498 has no significant effect on endogenous [Ca2+] responses in HEK293 cells produced by muscarinic acetylcholine receptor activation with carbachol or store-operated channel-mediated Ca2+ entry after depletion of intracellular stores with the Ca2+ pump inhibitor thapsigargin. SB705498 (10 pM-1 μM) also has no significant antagonist effect versus the close TRPV1 receptor paralog TRPV4 transiently expressed in HEK293 cells and activated using the synthetic ligand 4α-phorbol-12,13-didecanoate (10 μM). SB705498 reveals good antagonist potency against both the rat and guinea pig TRPV1. SB705498 antagonizes rat and guinea pig TRPV1 with pKi of 7.5 and 7.3, respectively. Coapplication of 100 nM to 10 μM SB705498 to the steady state of a maintained capsaicin response leads to rapid and complete inhibition of hTRPV1 at -70 mV. SB705498 inhibits capsaicin-mediated activation of hTRPV1 with IC50 of 3 nM and 17 nM at positive and negative holding potentials (-70 mV and + 70 mV), respectively. Coapplication of 1 μM SB705498 to the plateau period of the response produces complete and reversible inhibition of the TRPV1-mediated conductance. [1] SB705498 shows approximately equal activity versus multiple and diverse chemical and physical modes of TRPV1 receptor activation. SB705498 shows little or no activity versus a wide range of ion channels, receptors and enzymes. SB705498 produces full blockade of heat as well as pH activation of hTRPV1. [2]

In vivo SB705498 exhibits potent and reversible blockade against the multiple modes of TRPV1 activation, namely the vanilloid (capsaicin), heat- and acid-mediated activation of the receptor. SB705498 displays excellent activity at 10 and 30 mg/kg po with good reversal of allodynia. SB705498 is also shown to give 80% reversal of allodynia in the guinea pig FCA model at 10 mg/kg p.o.. [2]

Protocol

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.35 mM)
Ethanol 20 mg/mL (46.59 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.23
Formula

C17H16BrF3N4O

CAS No. 501951-42-4
Storage powder
in solvent
Synonyms N/A
Smiles FC(F)(F)C1=CN=C(C=C1)N2CCC(C2)NC(=O)NC3=CC=CC=C3Br

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01476098 Completed Drug: Placebo|Drug: SB-705498 Rhinitis GlaxoSmithKline April 2011 Phase 2
NCT01424397 Completed Drug: SB-705498|Drug: FP|Drug: placebo Rhinitis GlaxoSmithKline April 14 2011 Phase 2
NCT01424514 Completed Drug: SB-705498|Drug: Placebo Rhinitis GlaxoSmithKline December 1 2010 Phase 2
NCT01439308 Completed Drug: Placebo|Drug: SB-705498 Rhinitis GlaxoSmithKline December 2009 Phase 2
NCT00461682 Terminated Drug: SB-705498 Irritable Colon GlaxoSmithKline January 26 2007 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID