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

531492
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
847163-28-4C₁₅H₁₁N₃O

Products

Catalogue NumberPackaging Qty/Pack
5.31492.0001 Sklená flaša 10 mg
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
Catalogue Number GTIN
5.31492.0001 04055977260342

Documentation

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

Title

Safety Data Sheet (SDS) 

12/15-Lipoxygenase Inhibitor, ML351 - CAS 847163-28-4 - Calbiochem Certificates of Analysis

TitleLot Number
531492

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
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.