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531660 GCase Activator, NCGC00188758 - Calbiochem

GCase Activator, NCGC00188758 - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: N-(4-Ethynylphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-carboxamide, Glucocerebrosidase Activator, Glucocerebrosidase Chemical Chaperone, NCGC758

Primary Target: Glucocerebrosidase (Gcase)
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531660
Preis & Verfügbarkeit

Übersicht

Key Spec Table

Empirical Formula
C₁₇H₁₄N₄O

Preis & Verfügbarkeit

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      Description
      OverviewA cell-permeable pyrazolopyrimidine-carboxamide compound that directly binds to glucocerebrosidase (GCase; Kd ~ 9 µM for NT-467 fluorescent labeled GCase) and enhances its activity and serves as a chaperone for its translocation to the lysosomal compartment in fibroblasts of patients with Gaucher disease (AC50 = 5.2 and 6.5 µM for wild type and mutant N370S, respectively). Also shown to be effective in increasing GCase activity in macrophages from Gaucher's disease patients as well as in iPSC-derived macrophages (10.7 and 3.2 fold, respectively). Normalizes reactive oxygen species production and improves chemotaxis in Gaucher disease macrophages. Shown to permeate the blood-brain barrier. Exhibits desirable pharmacokinetic properties with plasma t1/2 = 19.3 h and Cmax of 1.03 µM (following a single injection of 50 mg/kg in mice).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531660
      Brand Family Calbiochem®
      SynonymsN-(4-Ethynylphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-carboxamide, Glucocerebrosidase Activator, Glucocerebrosidase Chemical Chaperone, NCGC758
      References
      ReferencesAflaki, E., et al. 2014. Sci. Transl. Med. 6, 240ra73.
      Patnaik, S., et al. 2012. J. Med. Chem. 55, 5734.
      Product Information
      FormLight orange powder
      Hill FormulaC₁₇H₁₄N₄O
      Chemical formulaC₁₇H₁₄N₄O
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetGlucocerebrosidase (Gcase)
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      5.31660.0001 04055977259988