538765 PDI Inhibitor IV, LOC14 - Calbiochem

538765
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₉N₃O₂S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38765.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, blood brain barrier permeable, orally bioavailable, non-toxic benzothiazolone derived compound that acts a potent, reversible and non-covalent inhibitor of protein disulfide isomerase (PDI) reductase activity (Kd = 61.7 nM for PDIa). Shown to bind to PDIa stoichiometrically (1:1), adjacent to the active site, and enforce PDI to adopt an oxidized conformation. Dose-dependently rescues both PC12 cells (EC50 = 500 nM) and medium spiny neurons from mutant huntingtin neurotoxicity. Exhibits favorable microsomal (k = 0.0016, t1/2 = 438.7 min, CLint = 0.17 ml/min/g mouse liver) and blood plasma stability (k = 0.0049, t1/2 = 144 min and 49.9% remains after 2 h incubation) and is well tolerated in mice (20 mg/kg, p.o.).

          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 Number538765
          Brand Family Calbiochem®
          Synonyms2-((4-(Cyclopropanecarbonyl)piperazin-1-yl)methyl)benzo[d]isothiazol-3(2H)-one, 2-((4-(Cyclopropylcarbonyl)-1-piperazinyl)methyl)-1,2-benzothiazol-3(2H)-one, Lead Optimized Compound 14, Protein Disulfide Isomerase Inhibitor IV
          DescriptionPDI Inhibitor IV, LOC14
          References
          ReferencesKaplan, A., et al. 2015. Proc. Natl. Acad. Sci. USA 112, In press.
          Product Information
          FormWhite solid
          Hill FormulaC₁₆H₁₉N₃O₂S
          Chemical formulaC₁₆H₁₉N₃O₂S
          ReversibleY
          Applications
          Biological Information
          Primary TargetPDI
          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 (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          PDI Inhibitor IV, LOC14 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Kaplan, A., et al. 2015. Proc. Natl. Acad. Sci. USA 112, In press.
          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.

          Revision09-September-2016 JSW
          Synonyms2-((4-(Cyclopropanecarbonyl)piperazin-1-yl)methyl)benzo[d]isothiazol-3(2H)-one, 2-((4-(Cyclopropylcarbonyl)-1-piperazinyl)methyl)-1,2-benzothiazol-3(2H)-one, Lead Optimized Compound 14, Protein Disulfide Isomerase Inhibitor IV
          DescriptionA cell-permeable, blood brain barrier permeable, orally bioavailable, non-toxic benzothiazolone derived compound that acts a potent, reversible and non-covalent inhibitor of protein disulfide isomerase (PDI) reductase activity (Kd = 61.7 nM for PDIa). Shown to bind to PDIa stoichiometrically (1:1), adjacent to the active site, and enforce PDI to adopt an oxidized conformation. Dose-dependently rescues both PC12 cells (EC50 = 500 nM) and medium spiny neurons from mutant huntingtin neurotoxicity. Exhibits favorable microsomal (k = 0.0016, t1/2 = 438.7 min, CLint = 0.17 ml/min/g mouse liver) and blood plasma stability (k = 0.0049, t1/2 = 144 min and 49.9% remains after 2 h incubation) and is well tolerated in mice (20 mg/kg, p.o.).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆H₁₉N₃O₂S
          Purity≥98% by HPLC
          SolubilityDMSO (25 mg/ml). Use only anhydrous DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
          Toxicity Standard Handling
          ReferencesKaplan, A., et al. 2015. Proc. Natl. Acad. Sci. USA 112, In press.