SB-705498

The transient receptor potential vanilloid type 1 (TRPV1) receptor is a nonselective cation channel gated by noxious heat, protons, and capsaicin (Cay-92350). 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).Formal Name: N-(2-bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]-urea. CAS Number: 501951-42-4. Molecular Formula: C17H16BrF3N4O. Formula Weight: 429.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 16 mg/ml, Ethanol: 10 mg/ml. lambdamax: 257, 312 nm. SMILES: BrC1=C(NC(N[C@@H]2CCN(C3=NC=C(C(F)(F)F)C=C3)C2)=O)C=CC=C1. InChi Code: InChI=1S/C17H16BrF3N4O/c18-13-3-1-2-4-14(13)24-16(26)23-12-7-8-25(10-12)15-6-5-11(9-22-15)17(19,20)21/h1-6,9,12H,7-8,10H2,(H2,23,24,26)/t12-/m1/s1. InChi Key: JYILLRHXRVTRSH-GFCCVEGCSA-N.