Chemical Property of SB-705498
Chemical Property:
- Boiling Point:506.9±50.0 °C(Predicted)
- PKA:13.00±0.20(Predicted)
- PSA：60.75000
- Density:1.59
- LogP:4.60570
- Storage Temp.:-20°C
- Solubility.:Soluble in DMSO (>25 mg/ml)
- XLogP3:3.8
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:6
- Rotatable Bond Count:3
- Exact Mass:428.04596
- Heavy Atom Count:26
- Complexity:493
- Purity/Quality:
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99%, *data from raw suppliers
1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)-2-pyridyl]pyrrolidin-3-yl]urea 97.0% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1CN(CC1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F
- Isomeric SMILES:C1CN(C[C@@H]1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F
- Recent ClinicalTrials:Intranasal SB-705498 in Allergic Rhinitis (AR) Patients
- Recent EU Clinical Trials:A randomized, double-blind, placebo controlled, incomplete block, 3 way cross over study in subjects with allergic rhinitis to assess the effect of intranasal repeat doses of SB-705498 when administered alone or in conjunction with intranasal fluticasone
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Description
The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin . 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). 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).
