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508317 | A740003 - CAS 861393-28-4 - Calbiochem

508317
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₃₀N₆O₃ 861393-28-4

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08317.0001
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          Glass bottle 5 mg
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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
          FormOff-white powder
          Hill FormulaC₂₆H₃₀N₆O₃
          Chemical formulaC₂₆H₃₀N₆O₃
          Structure formula Image
          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

          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.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number861393-28-4
          Chemical formulaC₂₆H₃₀N₆O₃
          Structure 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.