A tertiary sulfonamide-based compound that acts as a high-affinity oxytocin (OT) receptor-selective antagonist (Ki = 650 and 670pM in 125I-OVTA-competitive binding assays using human and rat OT-R, respectively), while displaying 65-, 245-, and 23,000-fold reduced affinity, respectively, toward human vassopressin receptors V1a, V2, and V1b. Shown to effectively inhibit OT- (10nM) induced Ca2+ mobilization in hOT-R-expressing HEK293-EBNA cells (IC50 = 14nM) in vitro and OT-stimulated uterine contractions in rats (1.4 -10mg/kg p.o. or 30mg/kg p.o.) in vivo. Product is supplied as a fumarate salt for enhanced aqueous solubility (20 and 10mg/ml, respectively, in water and HBSS).
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
