531492 12/15-Lipoxygenase Inhibitor, ML351 - Calbiochem

531492
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₅H₁₁N₃O

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      Glass bottle 10 mg
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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
      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

      Documentation

      12/15-Lipoxygenase Inhibitor, ML351 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Rai, G., et al. 2014. J. Med. Chem. 57, 4035.
      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.

      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
      Chemical formulaC₁₅H₁₁N₃O
      Purity≥97% by HPLC
      SolubilityDMSO (100 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
      ReferencesRai, G., et al. 2014. J. Med. Chem. 57, 4035.