JYL1421

JYL1421 is an antagonist of transient receptor potential vanilloid 1 (TRPV1). It inhibits calcium uptake induced by capsaicin (Cay-92350, Cay-10010743) in CHO cells expressing rat TRPV1 (EC50 = 9.2 nM). JYL1421 inhibits capsaicin-induced release of the neuropeptides somatostatin, substance P (Cay-24035), and calcitonin gene-related peptide (CGRP) from isolated rat trachea (IC50s = 227-491 nM). It inhibits capsaicin-induced hypothermia and hypotension in rats when administered at doses of 2 and 0.4 mg/kg, respectively. JYL1421 (2 mg/kg) also reduces the number of wiping movements induced by ocular administration of capsaicin in rats. Unlike several other TRPV1 antagonists, JYL1421 does not induce hyperthermia in rats when administered at doses ranging from 1.02 to 32.77 µmol/kg.Formal Name: N-[4-[[[[[[4-(1,1-dimethylethyl)phenyl]methyl]amino]thioxomethyl]amino]methyl]-2-fluorophenyl]-methanesulfonamide. CAS Number: 401907-26-4. Molecular Formula: C20H26FN3O2S2. Formula Weight: 423.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO:. lambdamax: 225 nm. SMILES: CC(C)(C)C1=CC=C(CNC(NCC2=CC(F)=C(NS(C)(=O)=O)C=C2)=S)C=C1. InChi Code: InChI=1S/C20H26FN3O2S2/c1-20(2,3)16-8-5-14(6-9-16)12-22-19(27)23-13-15-7-10-18(17(21)11-15)24-28(4,25)26/h5-11,24H,12-13H2,1-4H3,(H2,22,23,27). InChi Key: DUHBVFMCIJLUJX-UHFFFAOYSA-N.