532674 Dopamine D2 Receptor Antagonist, SB269652 - Calbiochem

532674
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₃₀N₄O

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      Glass bottle 10 mg
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      Description
      OverviewA tetrahydroisoquinoline-7-carbonitrile based compound that acts as a negative allosteric modulator of dopamine D2 receptor (estimated affinity (Kb) = 145-416 nM in GTP γS binding and in cell based functional assays). Its allosteric action requires D2R dimers. Shown to significantly reduce dopamine potency (8 to 16 fold), but acts as a partial antagonist and allows some dopamine action to remain. Displays features similar to orthosteric D2R antagonists and its highly stable tetrahydroisoquinoline (THIQ) moiety occupies the orthosteric site. Also exhibits bitopic mode of interaction with D2R. Binds to one promoter of D2R dimer in a bitopic mode and modulates the action of dopamine at the other. A G2A mutation in D2R causes a 9-fold reduction in its affinity and 5-fold decrease in negative cooperativity.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number532674
      Brand Family Calbiochem®
      SynonymsD2R antagonist, SB269652, SB-269652, SB 269652
      References
      ReferencesLane, J., et al. 2014. Nat. Chem. Biol. 10, 745.
      Product Information
      FormLight yellow solid
      Hill FormulaC₂₇H₃₀N₄O
      Chemical formulaC₂₇H₃₀N₄O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetD2
      Primary Target K<sub>i</sub>145-416 nM
      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 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

      Dopamine D2 Receptor Antagonist, SB269652 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Lane, J., et al. 2014. Nat. Chem. Biol. 10, 745.
      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.

      Revision20-November-2015 JSW
      SynonymsD2R antagonist, SB269652, SB-269652, SB 269652
      DescriptionA tetrahydroisoquinoline-7-carbonitrile based compound that acts as a negative allosteric modulator of dopamine D2 receptor (estimated affinity (Kb) = 145-416 nM in GTP γS binding and in cell based functional assays). Its allosteric action requires D2R dimers. Shown to significantly reduce dopamine potency (8 to 16 fold), but acts as a partial antagonist and allows some dopamine action to remain. Displays features similar to orthosteric D2R antagonists and its highly stable tetrahydroisoquinoline (THIQ) moiety occupies the orthosteric site. Also exhibits bitopic mode of interaction with D2R. Binds to one promoter of D2R dimer in a bitopic mode and modulates the action of dopamine at the other. A G2A mutation in D2R causes a 9-fold reduction in its affinity and 5-fold decrease in negative cooperativity.
      FormLight yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₃₀N₄O
      Purity≥97% by HPLC
      SolubilityDMSO (10 mg/ml)
      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
      ReferencesLane, J., et al. 2014. Nat. Chem. Biol. 10, 745.