531492 12/15-Lipoxygenase Inhibitor, ML351 - Calbiochem

531492
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₁N₃O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31492.0001
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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
          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.