ELN441958

ELN441958 is a bradykinin B1 receptor antagonist (Ki = 0. nM). It is selective for the bradykinin B1 receptor over a panel of greater than 100 enzymes and receptors at 10 µM but does bind to the µ-, delta-, and kappa-opioid receptors and M1 muscarinic receptor (Kis = 0. 0. 1. and 0. µM, respectively). ELN441958 inhibits calcium mobilization induced by the bradykinin B1 receptor agonist (Des-Arg10)-kallidin (DAKD) in IMR-90 cells expressing the human bradykinin B1 receptor (KB = 0. nM). It increases tail withdrawal latencies in a rhesus monkey model of carrageenan-induced hyperalgesia when administered at doses of 3 or 10 mg/kg. Formal Name: 7-chloro-2,3-dihydro-2-[3-[[9-(4-pyridinyl)-3,9-diazaspiro[5.5]undec-3-yl]carbonyl]phenyl]-1H-isoindol-1-one. CAS Number: 913064-47-8. Molecular Formula: C29H29ClN4O2. Formula Weight: 501.0. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml DMSO: Slightly soluble: 0.1-1 mg/ml. SMILES: O=C(N1CCC2(CC1)CCN(CC2)C3=CC=NC=C3)C4=CC=CC(N5CC6=C(C5=O)C(Cl)=CC=C6)=C4. InChi Code: InChI=1S/C29H29ClN4O2/c30-25-6-2-4-22-20-34(28(36)26(22)25)24-5-1-3-21(19-24)27(35)33-17-11-29(12-18-33)9-15-32(16-10-29)23-7-13-31-14-8-23/h1-8,13-14,19H,9-12,15-18,20H2. InChi Key: ARYQHSWJGHCGJS-UHFFFAOYSA-N. Storage: -20°C. Stability: > 4 years.