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504660 P2X Antagonist III - Calbiochem

P2X Antagonist III - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Purinergic Receptor P2X Antagonist III, N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

Primary Target: P2X₇
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504660
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₈H₃₂N₄O₂S

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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®
      SynonymsPurinergic Receptor P2X Antagonist III, N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
      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
      Quality LevelMQ100
      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

      P2X Antagonist III - Calbiochem 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
      SynonymsPurinergic Receptor P2X Antagonist III, N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
      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 Protect from light
      -20°C
      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.