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531492 12/15-Lipoxygenase Inhibitor, ML351 - CAS 847163-28-4 - Calbiochem

A cell-permeable, highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC50 = 200 nM for human).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 5-(Methylamino)-2-(naphthalen-1-yl)oxazole-4-carbonitrile, 12/15-LOX Inhibitor, 15-Lipoxygenase-1 Inhibitor

Primary Target: 12/15-LOX
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531492
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Tableau de caractéristiques principal

CAS #Empirical Formula
847163-28-4C₁₅H₁₁N₃O

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      Description
      OverviewA cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC50 = 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC50 > 50 µM), 12-LOX (IC50 > 100 µM), and 15-LOX (IC50 > 100 µM) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µM). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t1/2 ~ 1 h in both plasma and brain; Cmax of 13.8 and 28.8 µM in plasma and brain, respectively; at 30 mg/kg, i.p).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531492
      Brand Family Calbiochem®
      Synonyms5-(Methylamino)-2-(naphthalen-1-yl)oxazole-4-carbonitrile, 12/15-LOX Inhibitor, 15-Lipoxygenase-1 Inhibitor
      References
      ReferencesRai, G., et al. 2014. J. Med. Chem. 57, 4035.
      Product Information
      CAS number847163-28-4
      FormYellow powder
      Hill FormulaC₁₅H₁₁N₃O
      Chemical formulaC₁₅H₁₁N₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Target12/15-LOX
      Purity≥97% 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
      Global Trade Item Number
      Référence GTIN
      5.31492.0001 04055977260342

      Documentation

      12/15-Lipoxygenase Inhibitor, ML351 - CAS 847163-28-4 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      12/15-Lipoxygenase Inhibitor, ML351 - CAS 847163-28-4 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      531492

      Références bibliographiques

      Aperçu de la référence bibliographique
      Rai, G., et al. 2014. J. Med. Chem. 57, 4035.
      Fiche technique

      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.

      Revision29-August-2014 JSW
      Synonyms5-(Methylamino)-2-(naphthalen-1-yl)oxazole-4-carbonitrile, 12/15-LOX Inhibitor, 15-Lipoxygenase-1 Inhibitor
      DescriptionA cell-permeable, non-toxic naphthyl-oxazole compound that acts as a highly potent, selective, active site directed, mixed type inhibitor of lipoxygenase-12/15 (IC50 = 200 nM for human). The inhibition appears to be non-reductive and reversible in nature. Displays excellent selectivity over 5-LOX (IC50 > 50 µM), 12-LOX (IC50 > 100 µM), and 15-LOX (IC50 > 100 µM) and does not affect the activity of COX-1 and -2 in any significant manner (<10% inhibition at 15 µM). Can cross the blood brain barrier (brain to plasma ratio = 2.8). Offers protection against glutamate-induced oxidative toxicity in mouse neuronal HT22 cells and reduces the size of infarcts in a murine model of ischemic stroke. Displays good aqueous stability over a wide range of pH. Exhibits attractive pharmacokinetic properties (t1/2 ~ 1 h in both plasma and brain; Cmax of 13.8 and 28.8 µM in plasma and brain, respectively; at 30 mg/kg, i.p).
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number847163-28-4
      Chemical formulaC₁₅H₁₁N₃O
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesRai, G., et al. 2014. J. Med. Chem. 57, 4035.