534377 CMB-087229 - Calbiochem

534377
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₀H₈Cl₂N₂O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.34377.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, blood-brain barrier permeable, non-toxic pyrazolone compound that potently blocks mutant Cu/Zn SOD1 cytotoxicity (EC50 = 67 nM in PC12 cells expressing mutant G93A SOD1). Shown to directly interact with 26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1 and enhance proteasome activity. Offers neuroprotection against protein aggregation induced toxicity and prolongs the survival of ALS transgenic mice by 13.3% (20 mg/kg, i.p., q.d.) Demonstrates attractive microsomal (T1/2 = 93 & 36 min in human & mouse, respectively) and metabolic stability, aqueous solubility (250 µM) and PK profile in mice. Poorly affects the activities of 68-enzymes & receptors, hERG and Cyp450 isozymes at 10 µM.

          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 Number534377
          Brand Family Calbiochem®
          Synonyms5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
          References
          ReferencesTripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
          Chen, T., et al. 2012. J. Med. Chem. 55, 515.
          Product Information
          FormWhite solid
          Hill FormulaC₁₀H₈Cl₂N₂O₂
          Chemical formulaC₁₀H₈Cl₂N₂O₂
          ReversibleY
          Applications
          Biological Information
          Primary Target26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1
          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 Ambient Temperature Only
          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

          CMB-087229 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Tripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
          Chen, T., et al. 2012. J. Med. Chem. 55, 515.
          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.

          Revision28-July-2017 JSW
          Synonyms5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
          DescriptionA cell-permeable, blood-brain barrier permeable, non-toxic pyrazolone compound that potently blocks mutant Cu/Zn SOD1 cytotoxicity (EC50 = 67 nM in PC12 cells expressing mutant G93A SOD1). Shown to directly interact with 26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1 and enhance proteasome activity. Offers neuroprotection against protein aggregation induced toxicity and prolongs the survival of ALS transgenic mice by 13.3% (20 mg/kg, i.p., q.d.) Demonstrates attractive microsomal (T1/2 = 93 & 36 min in human & mouse, respectively) and metabolic stability, aqueous solubility (250 µM) and PK profile in mice. Poorly affects the activities of 68-enzymes & receptors, hERG and Cyp450 isozymes at 10 µM.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₀H₈Cl₂N₂O₂
          Purity≥98% 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
          ReferencesTripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
          Chen, T., et al. 2012. J. Med. Chem. 55, 515.