116765 | Adenosine A2A/A₁ Receptor Antagonist - Calbiochem

116765
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₃H₂₂N₄O₃ •2HCl

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      US1116765-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA blood-brain barrier-permeant indenopyrimidinone that acts as a dual A1/A2A antagonist (Ki = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A1- or A2A-expressing CHO-K1 cells) and effectively reverses D2 antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both rats and mice (ED50 = 0.3 and <0.1 mg/kg, respectively) in vivo by simultaneously reversing A1-mediated inhibition of DA (Dopamine) release and A2A-dependent inhibition of D2 receptor response to DA.
          Catalogue Number116765
          Brand Family Calbiochem®
          Synonyms2-Amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]-pyrimidin-5-one, diHCl
          References
          ReferencesShook, B.C., et al. 2012. J. Med. Chem. 55, 1402.
          Product Information
          FormLight yellow solid
          Hill FormulaC₂₃H₂₂N₄O₃ •2HCl
          Chemical formulaC₂₃H₂₂N₄O₃ •2HCl
          Hygroscopic Hygroscopic
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥97% 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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          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

          Certificates of Analysis

          TitleLot Number
          116765

          References

          Reference overview
          Shook, B.C., et al. 2012. J. Med. Chem. 55, 1402.
          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.

          Revision24-September-2012 JSW
          Synonyms2-Amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno[1,2-d]-pyrimidin-5-one, diHCl
          DescriptionA blood-brain barrier-permeant indenopyrimidinone compound that acts as a dual A1/A2A antagonist (Ki = 48.2 and 6.5 nM, respectively, against agonist-induced cAMP response in A1- or A2A-expressing CHO-K1 cells) and effectively reverses neuroleptic D2 receptor antagonist haloperidol- (1 mg/kg; s.c.) induced catalepsy in both mice (by 85% and 100%, respectively, with 0.1 mg/kg or 1 mg/kg oral dosage 30 min after haloperidol) and rats (by 88% and 97%, respectively, with 1 mg/kg or 10 mg/kg oral dosage) in vivo by simultaneously reversing A1-mediated inhibition of DA (Dopamine) release and A2A-dependent inhibition of D2 receptor response to DA.
          FormLight yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₂₂N₄O₃ •2HCl
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (10 mg/ml; clear, yellow solution)
          Storage +2°C to +8°C
          Hygroscopic
          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
          ReferencesShook, B.C., et al. 2012. J. Med. Chem. 55, 1402.