500106 Oxytocin Receptor Antagonist, MSC1630296 - Calbiochem

500106
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500106-2MG
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      Glass bottle 2 mg
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      Description
      OverviewA tertiary sulfonamide-based compound that acts as a high-affinity oxytocin (OT) receptor-selective antagonist (Ki = 650 and 670 pM 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- (10 nM) induced Ca2+ mobilization in hOT-R-expressing HEK293-EBNA cells (IC50 = 14 nM) in vitro and OT-stimulated uterine contractions in rats (1.4 -10 mg/kg p.o. or 30 mg/kg p.o.) in vivo. Product is supplied as a fumarate salt for enhanced aqueous solubility (20 and 10 mg/ml, respectively, in water and HBSS).
      Catalogue Number500106
      Brand Family Calbiochem®
      SynonymsOT-R Antagonist, 3-(4-(N-(4-chlorophenyl)-N-(2-oxo-2-(2-(2-oxoindolin-3-ylidene)hydrazinyl)ethyl)sulfamoyl)phenyl)-N-(3-(dimethylamino)propyl)propanamide, fumarate salt
      References
      ReferencesQuattropani, A., et al. 2005. J Med Chem. 48, 7882.
      Product Information
      FormBrown solid
      Hill FormulaC₃₀H₃₃ClN₆O₅S.C₄H₄O₄
      Chemical formulaC₃₀H₃₃ClN₆O₅S.C₄H₄O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetOxytocin receptor
      Primary Target K<sub>i</sub>0.65 nM
      Purity≥93% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Quattropani, A., et al. 2005. J Med Chem. 48, 7882.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision11-March-2013 JSW
      SynonymsOT-R Antagonist, 3-(4-(N-(4-chlorophenyl)-N-(2-oxo-2-(2-(2-oxoindolin-3-ylidene)hydrazinyl)ethyl)sulfamoyl)phenyl)-N-(3-(dimethylamino)propyl)propanamide, fumarate salt
      DescriptionA tertiary sulfonamide-based compound that acts as a high-affinity oxytocin (OT) receptor-selective antagonist (Ki = 650 and 670 pM in 125I-OVTA-competitive binding assays using human and rat OT-R, respectively) and effectively inhibits OT- (10 nM) induced Ca2+ mobilization in hOT-R-expressing HEK293-EBNA cells (IC50 = 14 nM), displaying 65-, 245-, and 23,000-fold reduced affinity, respectively, toward human vassopressin receptors V1a (in 125I-LVA-competitive V1a binding assays), V2, and V1b (in [3H]AVP-competitive binding assays). Shown to effectively block OT-stimulated uterine contractions in non-pregnant rats (by 50% and 72% via i.p. dose of 1.4 mg/kg and 10 mg/kg, respectively; max. inhibition = 35% with 30 mg/kg oral dosing), as well as spontaneous uterine contractions in late-term pregnant rats (29% inhibition; 30 mg/kg p.o.) in vivo. Product is supplied as a fumarate salt for enhanced aqueous solubility (20 and 10 mg/ml, respectively, in water and HBSS).
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₀H₃₃ClN₆O₅S.C₄H₄O₄
      Structure formulaStructure formula
      Purity≥93% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesQuattropani, A., et al. 2005. J Med Chem. 48, 7882.