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530463 Dopamine Receptor D3 Antagonist II, YQA14 - Calbiochem

A highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (Ki = 0.0680 pM high affinity and 2.11 nM low affinity).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: D3R Antagonist

Primary Target: D3
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₃H₂₇ClN₄O₃
      Description
      Overview

      This product has been discontinued.



      An orally bioavailable benzoxazolone carboxamide derivative that acts as a highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (Ki = 0.0680 pM high affinity and 2.11 nM low affinity). Displays >150-fold greater selectivity for D3 over D2 receptors and about 1000-fold selectivity over other dopamine receptors. Exhibits strong anti-addiction profile and reduces self administration of cocaine in rodent models (6.25 to 25 mg/kg in rats) without affecting their sucrose water self-administration and locomotor activity.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530463
      Brand Family Calbiochem®
      SynonymsD3R Antagonist
      References
      ReferencesSong, R., et al. 2014. Neuropharm. 77, 398.
      Song, R., et al. 2011. Addiction Biol. 17, 259.
      Product Information
      FormTan powder
      Hill FormulaC₂₃H₂₇ClN₄O₃
      Chemical formulaC₂₃H₂₇ClN₄O₃
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetD3
      Primary Target K<sub>i</sub>0.068 pM
      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 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
      Global Trade Item Number
      Catalogue Number GTIN
      530463 0

      Documentation

      Dopamine Receptor D3 Antagonist II, YQA14 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Song, R., et al. 2014. Neuropharm. 77, 398.
      Song, R., et al. 2011. Addiction Biol. 17, 259.
      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.

      Revision06-June-2014 JSW
      SynonymsD3R Antagonist
      DescriptionAn orally bioavailable benzoxazolone carboxamide derivative that acts as a highly potent and selective antagonist of dopamine D3 receptors. Has two binding sites on human cloned D3 receptors (Ki = 0.0680 pM high affinity and 2.11 nM low affinity). Displays >150-fold greater selectivity for D3 over D2 receptors and about 1000-fold selectivity over other dopamine receptors. Exhibits strong anti-addiction profile and reduces self administration of cocaine in rodent models (6.25 to 25 mg/kg in rats) without affecting their sucrose water self-administration and locomotor activity.
      FormTan powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₂₇ClN₄O₃
      Purity≥98% by HPLC
      SolubilityDMSO (100 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
      ReferencesSong, R., et al. 2014. Neuropharm. 77, 398.
      Song, R., et al. 2011. Addiction Biol. 17, 259.