532978 | PLD2 Inhibitor, ML395 - Calbiochem

532978
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₆H₂₉N₅O₂

      Pricing & Availability

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      5.32978.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC50 = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC50 = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski's rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC50 = 3.9 µM, CYP2D6 IC50 =16.4 µM, CYP1A2 IC50>30 µM, and CYP2C9 IC50>30 µM).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number532978
          Brand Family Calbiochem®
          SynonymsPhosppolipase D2 inhibitor, VU0468809, ML-395
          References
          ReferencesO'Reilly, M.C., et al. 2014. ChemMedChem 9, 2633.
          Product Information
          FormOff-white solid
          Hill FormulaC₂₆H₂₉N₅O₂
          Chemical formulaC₂₆H₂₉N₅O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetPLD2
          Primary Target IC<sub>50</sub>360 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

          References

          Reference overview
          O'Reilly, M.C., et al. 2014. ChemMedChem 9, 2633.

          Technical Info

          Title
          Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System
          White Paper: Further considerations of antibody validation and usage.
          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.

          Revision17-April-2015 JSW
          SynonymsPhosppolipase D2 inhibitor, VU0468809, ML-395
          DescriptionA cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC50 = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC50 = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski's rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC50 = 3.9 µM, CYP2D6 IC50 =16.4 µM, CYP1A2 IC50>30 µM, and CYP2C9 IC50>30 µM).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₆H₂₉N₅O₂
          Purity≥97% by HPLC
          SolubilityDMSO (50 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
          ReferencesO'Reilly, M.C., et al. 2014. ChemMedChem 9, 2633.