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505418 AF353 - CAS 927887-18-1 - Calbiochem

505418
  
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      Overview

      Replacement Information

      Key Specifications Table

      CAS #Empirical Formula
      927887-18-1C₁₄H₁₈ClIN₄O₂
      Description
      OverviewA novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10 nM to 1 µM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min).
      Catalogue Number505418
      Brand Family Calbiochem®
      SynonymsP2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353
      Application Data
      References
      ReferencesGever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.
      Product Information
      CAS number927887-18-1
      FormLight brown powder
      Hill FormulaC₁₄H₁₈ClIN₄O₂
      Chemical formulaC₁₄H₁₈ClIN₄O₂
      ReversibleY
      Applications
      Biological Information
      Primary TargetP2X3
      Purity≥99% 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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      AF353 - CAS 927887-18-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Gever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.
      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.

      Revision30-August-2013 JSW
      SynonymsP2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353
      Application Data
      DescriptionA novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10 nM to 1 µM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min).
      FormLight brown powder
      CAS number927887-18-1
      Chemical formulaC₁₄H₁₈ClIN₄O₂
      Purity≥99% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesGever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.