504660 | P2X Antagonist III - Calbiochem

504660
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₈H₃₂N₄O₂S

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04660.0001
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          Glass bottle 10 mg
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          Description
          OverviewA phenylthio-nicotinamide that acts as a high affinity P2X7 antagonist (pKi = 8.7 and 7.9, respectively, against 30 nM A-804598 for rat and human P2X7 binding) and potently inhibits P2X7-dependent cellular Ca2+ mobilization (pIC50 = 8.3, 7.5, and 7.2, respectively, using 1321N1 expressing human, mouse, or rat P2X7; drug added 0.5 h prior to 3 min 0.25 mM BzATP stimulation), while exhibiting much reduced or little potency toward a panel of 50 ion channels, transporters, and receptors. Although not suitable for oral dosing due to high hepatic extraction ratios, effective delivery and brain P2X7 occupancy can be achieved via s.c. dosing in rats (30 mg/kg) in vivo.
          Catalogue Number504660
          Brand Family Calbiochem®
          SynonymsN-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide, Purinergic Receptor P2X Antagonist III
          References
          ReferencesLetavic, M. A., et al. 2013. Br. J. Pharmacol. 4, 419.
          Product Information
          FormWhite powder
          Hill FormulaC₂₈H₃₂N₄O₂S
          Chemical formulaC₂₈H₃₂N₄O₂S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetP2X₇
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage -20°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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Letavic, M. A., et al. 2013. Br. J. Pharmacol. 4, 419.
          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.

          Revision09-August-2013 JSW
          SynonymsN-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide, Purinergic Receptor P2X Antagonist III
          DescriptionA phenylthio-nicotinamide that acts as a high affinity P2X7 antagonist (pKi = 8.7 and 7.9, respectively, against 30 nM A-804598 for rat and human P2X7 binding) and potently inhibits P2X7-dependent cellular Ca2+ mobilization (pIC50 = 8.3, 7.5, and 7.2, respectively, using 1321N1 expressing human, mouse, or rat P2X7; drug added 0.5 h prior to 3 min 0.25 mM BzATP stimulation) and IL-1β secretion (pIC50 = 7.6; drug added 0.5 h prior to 1.5 h 0.5 mM BzATP stimulation of LPS-activated human PBMC), while exhibiting much reduced or little potency toward a panel of 50 ion channels, transporters, and receptors (pIC50 <6). Although not suitable for oral dosing due to high hepatic extraction ratios (>0.92 in human, mouse, and rat), effective delivery (tmax = 15 min & Cmax ~8.5 µg/mL in plasma and brain; 30 mg/kg s.c.) and brain P2X7 occupancy (>50% and >80% at tmax following s.c. dose of 3.2 mg/kg and 32 mg/kg, respectively) can be achieved via s.c. dosing in rats in vivo.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₈H₃₂N₄O₂S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage -20°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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesLetavic, M. A., et al. 2013. Br. J. Pharmacol. 4, 419.