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508317 A740003 - CAS 861393-28-4 - Calbiochem

508317
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Empirical FormulaCAS #
C₂₆H₃₀N₆O₃ 861393-28-4

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      Description
      OverviewA highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC50 = 18 nM and 40 nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10 µM concentrations. Blocks agonist-evoked IL-1b release (IC50 = 156 nM) and pore formation (IC50 = 92 nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund′s adjuvant -induced thermal hyperalgesia (ED50 = 38-54 mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve.
      Catalogue Number508317
      Brand Family Calbiochem®
      SynonymsN-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
      References
      ReferencesHonore, P., et al. 2006. J. Pharmacol. Exp. Ther. 319, 1376.
      Product Information
      CAS number861393-28-4
      FormWhite to yellow to light brown powder
      Hill FormulaC₂₆H₃₀N₆O₃
      Chemical formulaC₂₆H₃₀N₆O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetP2X7
      Primary Target IC<sub>50</sub>18 nM
      Purity≥98% 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

      A740003 - CAS 861393-28-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Honore, P., et al. 2006. J. Pharmacol. Exp. Ther. 319, 1376.
      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.

      Revision25-October-2013 JSW
      SynonymsN-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide, A 740003, P2X7 Purinegic Receptor, A740003, A740003
      DescriptionA highly potent, selective, competitive antagonist of P2X7 purinegic receptor (IC50 = 18 nM and 40 nM, respectively as measured by Bz-ATP-stimulated Ca2+ flux). Does not affect other P2 receptors even at 10 µM concentrations. Blocks agonist-evoked IL-1b release (IC50 = 156 nM) and pore formation (IC50 = 92 nM) in differentiated human THP-1 cells. Also shown to reduce carrageenan and Freund′s adjuvant -induced thermal hyperalgesia (ED50 = 38-54 mg/kg, i.p) and neuropathic pain induced by chronic constriction injury (CIC) of the sciatic nerve.
      FormWhite to yellow to light brown powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number861393-28-4
      Chemical formulaC₂₆H₃₀N₆O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (30 mg/ml). Slight warming is required for complete solubilization.
      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
      ReferencesHonore, P., et al. 2006. J. Pharmacol. Exp. Ther. 319, 1376.