500106 Oxytocin Receptor Antagonist, MSC1630296 - Calbiochem

500106
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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.