SB-366791

• CAT Number: I003637
• CAS Number: 472981-92-3
• Molecular Formula: C16H14ClNO2
• Molecular Weight: 287.7
• Purity: ≥95%
• Target: TRP Channel
• Solubility: Soluble to 10 mM in ethanol and to 100 mM in DMSO
• Storage: Store at RT
• IC50: 5.7±1.2 nM
• InChI: InChI=1S/C16H14ClNO2/c1-20-15-4-2-3-14(11-15)18-16(19)10-7-12-5-8-13(17)9-6-12/h2-11H,1H3,(H,18,19)/b10-7+
• InChIKey: RYAMDQKWNKKFHD-JXMROGBWSA-N
• SMILES: ClC1=CC=C(/C=C/C(NC2=CC(OC)=CC=C2)=O)C=C1

SB-366791 is a potent , competitive and selective vanilloid receptor (VR1/TRPV1) antagonist with IC50 of 5.7±1.2 nM.

SB-366791 produced a concentration-dependent inhibition of the response to capsaicin with an apparent pKb of 7.74±0.08. Schild analysis indicated a competitive mechanism of action with a pA2 of 7.71.[1] SB-366791 showed a concentration-dependent potentiation of pH 5-induced 45Ca2+uptake in CHO cells expressing rat TRPV1 but not in untransfected cells[2]

Reference

1:TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Lappin SC, Randall AD, Gunthorpe MJ, Morisset V.Eur J Pharmacol. 2006 Jul 1;540(1-3):73-81. Epub 2006 May 6. PMID: 16737693 2:Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Gunthorpe MJ, Rami HK, Jerman JC, Smart D, Gill CH, Soffin EM, Luis Hannan S, Lappin SC, Egerton J, Smith GD, Worby A, Howett L, Owen D, Nasir S, Davies CH, Thompson M, Wyman PA, Randall AD, Davis JB.Neuropharmacology. 2004 Jan;46(1):133-49. Erratum in: Neuropharmacology. 2004 May;46(6):905. PMID: 14654105