1. Membrane Transporter/Ion Channel
  2. TRP Channel

SB-705498 

Cat. No.: HY-10633 Purity: 99.73%
Data Sheet SDS Handling Instructions

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

For research use only. We do not sell to patients.
SB-705498 Chemical Structure

SB-705498 Chemical Structure

CAS No. : 501951-42-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $150 In-stock
50 mg $650 In-stock
100 mg $1050 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1.

IC50 & Target

pIC50: 7.1

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 (10 mg/kg p.o.) gives 80% reversal of allodynia in the guinea pig FCA model[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00269022 GlaxoSmithKline Migraine, Acute January 2006 Phase 2
NCT01476098 GlaxoSmithKline Rhinitis April 2011 Phase 2
NCT01424514 GlaxoSmithKline Rhinitis December 2010 Phase 2
NCT01439308 GlaxoSmithKline Rhinitis December 2009 Phase 2
NCT00281684 GlaxoSmithKline Toothache December 2005 Phase 2
NCT00461682 GlaxoSmithKline Irritable Colon January 26, 2007 Phase 2
NCT00731250 GlaxoSmithKline Rhinitis July 22, 2008 Phase 1
NCT01424397 GlaxoSmithKline Rhinitis April 2011 Phase 2
NCT00907933 GlaxoSmithKline Rhinitis November 10, 2008 Phase 1
NCT01673529 GlaxoSmithKline Dermatitis, Atopic July 17, 2012 Phase 1
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References
Molecular Weight

429.23

Formula

C₁₇H₁₆BrF₃N₄O

CAS No.

501951-42-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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SB-705498
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HY-10633
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