538285 Glucosylceramide Synthase Inhibitor, Genz-123346 - CAS 491833-30-8 - Calbiochem

538285
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₃₈N₂O₄ 491833-30-8

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      5.38285.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, orally bioavailable fatty acid amide derivative that acts as a highly potent and specific inhibitor of Glucosylceramide Synthase (GL1 synthase; IC50 = 14 nM for ganglioside GM1 inhibition). Does not affect the activities of other related glycosidase, such as 1-O-acylceramide synthase, a-glucosidase, and glucocerebrosidase in any significant manner. Shown to improve glucose tolerance, improve insulin sensitivity, and normalize hemoglobin A1C levels in Zucker diabetic fatty rats (75 mg/kg/day, p.o. for 6 weeks). Also acts as an inhibitor of GlcCer synthase and blocks the conversion of ceramide to GlcCer in murine models that are orthologous to human autosomal dominant polycystic kidney disease and nephronophthisis. Diminishes Akt-mTOR signaling by reducing phosphorylation of Akt and ribosomal S6 kinase in HEK293T cells without affecting their total levels.

          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 Number538285
          Brand Family Calbiochem®
          Synonyms(1R,2R)-nonanoic acid[2-(2ʹ,3ʹ-dihydro-benzo [1, 4] dioxin-6ʹ-yl)-2-hydroxy-1-pyrrolidin-1-ylmethyl-ethyl]-amide, GL1 synthase Inhibitor, Genz-123346, Genz123346
          References
          ReferencesShen, W., et al. 2014. J. Neurochem. 129, 884.
          Natoli, T.A., et al. 2010. Nat. Med. 16, 788.
          Zhao, H., et al. 2007. Diabetes. 56, 1210.
          Product Information
          CAS number491833-30-8
          FormWhite to off-white solid
          Hill FormulaC₂₄H₃₈N₂O₄
          Chemical formulaC₂₄H₃₈N₂O₄
          ReversibleY
          Applications
          Biological Information
          Primary Targetglucosylceramide synthase
          Primary Target IC<sub>50</sub>14 nM for ganglioside GM1 suppression
          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, Blue Ice or Dry Ice
          Toxicity Standard Handling
          Storage -20°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

          Glucosylceramide Synthase Inhibitor, Genz-123346 - CAS 491833-30-8 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Shen, W., et al. 2014. J. Neurochem. 129, 884.
          Natoli, T.A., et al. 2010. Nat. Med. 16, 788.
          Zhao, H., et al. 2007. Diabetes. 56, 1210.
          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
          Synonyms(1R,2R)-nonanoic acid[2-(2ʹ,3ʹ-dihydro-benzo [1, 4] dioxin-6ʹ-yl)-2-hydroxy-1-pyrrolidin-1-ylmethyl-ethyl]-amide, GL1 synthase Inhibitor, Genz-123346, Genz123346
          DescriptionA cell-permeable, orally bioavailable fatty acid amide derivative that acts as a highly potent and specific inhibitor of Glucosylceramide Synthase (GL1 synthase; IC50 = 14 nM for ganglioside GM1 inhibition). Does not affect the activities of other related glycosidase, such as 1-O-acylceramide synthase, a-glucosidase, and glucocerebrosidase in any significant manner. Shown to improve glucose tolerance, improve insulin sensitivity, and normalize hemoglobin A1C levels in Zucker diabetic fatty rats (75 mg/kg/day, p.o. for 6 weeks). Also acts as an inhibitor of GlcCer synthase and blocks the conversion of ceramide to GlcCer in murine models that are orthologous to human autosomal dominant polycystic kidney disease and nephronophthisis. Diminishes Akt-mTOR signaling by reducing phosphorylation of Akt and ribosomal S6 kinase in HEK293T cells without affecting their total levels.
          FormWhite to off-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number491833-30-8
          Chemical formulaC₂₄H₃₈N₂O₄
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°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
          ReferencesShen, W., et al. 2014. J. Neurochem. 129, 884.
          Natoli, T.A., et al. 2010. Nat. Med. 16, 788.
          Zhao, H., et al. 2007. Diabetes. 56, 1210.