532674 Dopamine D2 Receptor Antagonist, SB269652 - Calbiochem

532674
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₃₀N₄O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32674.0001
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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
          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.